`
`Paul J. Reider, Ph.D.
`United States of America Citizenship
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`HOME
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`BUSINESS
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` 377 Walnut Lane
`Princeton University
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`Princeton, NJ 08540
`Department of Chemistry
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` (609) 924-4365 (home)
`Frick Laboratory
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` (805) 795-7800 (cell)
`Princeton, NJ 08544
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`(609) 258-5027
`e-mail: preider@princeton.edu
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`EMPLOYMENT HISTORY
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`From – To
`7/15 - present
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`8/08-7/15
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`From – To
`4/02 – 11/07
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`From – To
`2/95 - 4/02
`2/91 - 1/95
`5/89 - 2/91
`1/87 - 5/89
`5/84 - 12/86
`9/80 - 5/84
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`Degree
`A. B.
`Ph.D.
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`PRINCETON UNIVERSITY
`Lecturer at the Rank of Professor
`Department of Chemistry
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`Pharmaceutical Specialist &
`Lecturer
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`Department of Chemistry
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`AMGEN, INC.
`Vice President,
`Chemistry Research & Discovery
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`MERCK/MRL
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`Vice President, Process Research
`Executive Director
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`Director
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`Assistant Director
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`Research Fellow
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`Senior Research Chemist
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`EDUCATION
`Date
`School
`1972
`Washington Square College (NYU)
`1978
`University of Vermont
`Colorado State University 1978-1980
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`ACADEMIC AND PROFESSIONAL HONORS
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`17. 2011 National Academy of Sciences Award for Chemistry in Service to Society (May 2011)
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`Major/Minor/Courses
`Psychology/Chemistry
`Organic Chemistry
`NIH Postdoctoral Fellow
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`CFAD v. Anacor, IPR2015-01776 ANACOR EX. 2030 - 1/26
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`16. B. R. Baker Memorial Lecturer of 2006 – June 2006
`15. Earle B. Barnes Award for Leadership in Chemical Research (ACS National Award) -2003
`14. Novartis Chemistry Lectureship – 2003
`13. Senior Editor – “Science of Synthesis” -- 2003 -- present
`12. Prix Galien 2000 Innovative Product Award – June 2000 (Singulair™)
`11. Prix Galien 2000 Research Team Award- June 2000 (Singulair™)
`10. Merck Board of Directors Scientific Award – 1998 (Crixivan™)
` 9.
`Senior Editor - "Current Opinion in Drug Discovery & Development"
` 8. National Research Council - Board of Chemical Sciences & Technology (1998-2001)
` 7. Herman S. Bloch Memorial - University of Chicago – 1996
` 6. Chair - 1996 Gordon Research Conference - Heterocyclic Compounds
` 5. Vice Chair - 1995 Gordon Research Conference - Heterocyclic Compounds
` 4. NSF Workshop on Synthesis July 1988
` 3. MRL Ambassador Program (to Colorado State University) (1982-1990)
` 2. Merck Speakers List (1982 - 2002)
` 1. National Research Service Award (NIH Postdoctoral Fellow) 1979-1980
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`EDITORIAL AND ADVISORY BOARDS
` 12. Medicines for Malaria Venture -- Expert Scientifc Advisory Committee -2010 -- present
` 11. TB Alliance -- Scientific Advisory Committee - 2010 - present
` 10. Emory Institute For Drug Discovery – Advisory Board - 2009 – 2013
` 9. Tetraphase Pharmaceuticals -- Scientific Advisor 2009 -- present
` 8. Satori Pharmaceuticals -- Advisory Board -- 2009 -- 2013
` 7. Chemical & Engineering News Advisory Board – 2006 to 2009
` 6. ACS Executive Directors’ 2010 Committee – 2004 to present
` 5. Steering Committee BCST – Challenges for the Chemical Sciences in the 21st Century –
`2003
` 4. Steering Committee & BCST – Challenges for the Chemical Sciences in the 21st Century –
` Workshop on Health and Medicine (National Research Council) – 2002
` 3. Editorial Advisory Board – “Journal Organic Chemistry”
` 2. Editorial Advisory Board - "Organic Letters"
` 1. Editorial Advisory Board – Journal of the American Chemical Society
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`ACADEMIC VISITING COMMITTEES
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`3. Chemical Engineering Advisory Board, University of California Santa Barbara
`2. Member – California Institute of Technology Division of Chemistry & Chemical Engineering
`1. Harvard Overseers’ Committee to Visit the Department of Chemistry & Chemical Biology
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`PUBLICATIONS
` 181. Targeting NAD+ Metabolism in the Human Malaria Parasite Plasmodium falciparum
`Jessica K. O'Hara, Lewis J. Kerwin, Simon A. Cobbold, Jonathan Tai, Thomas A. Bedell, Paul J. Reider,
`Manuel Llinás; PLoS ONE; 2014 April; 9(4):e94061
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`180. Highly Loaded Nanoparticulate formulation of Progesterone for Emergency Traumatic brain
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`Injury Treatment; Carlos E. Figueroa, Paul J. Reider, Panee Burckel, A. Alan Pinkerton &
`Robert K. Prud’homme; Therapeutic Delivery; 2012, 3 (11), p.1269
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`179. A Concise and Convergent Synthesis of PA-824 Maurice A. Marsini, Paul J. Reider*, and Erik
`J. Sorensen*; J. Org. Chem., 2010, 75 (21), pp 7479–7482
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`178. Stereoselective Synthesis of anti-N-Protected 3-Amino-1,2-epoxides by Nucleophilic Addition to
`N-tert-Butanesulfinyl Imine of a Glyceraldehyde Synthon† Scott S. Harried, Michael D.
`Croghan, Matthew R. Kaller, Patricia Lopez, Wenge Zhong, Randall Hungate and Paul J.
`Reider J. Org. Chem., 2009, 74 (16), pp 5975–5982
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`177. “Practical synthesis of the calcimimetic agent, cinacalcet”, Tetrahedron Letters, (2008), 49(1), 13,
`Oliver R. Thiel, , Charles Bernard, Wanda Tormos, Alan Brewin, Shuji Hirotania, Kazuo
`Murakamia, Kenji Saitoa, Robert D. Larsena, Michael J. Martinellia and Paul J. Reidera
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`176. “Design, Synthesis, and Biological Evaluation of Potent c-Met Inhibitors”, J. Med.Chem,
` (2008), 51 (18), 5766–5779, Noel D. D’Angelo*†, Steven F. Bellon‡, Shon K. Booker†, Yuan
` Cheng†, Angela Coxon§, Celia Dominguez†, Ingrid Fellows†, Douglas Hoffman∥, Randall
` Hungate†, Paula Kaplan-Lefko§, Matthew R. Lee‡, Chun Li⊥, Longbin Liu†, Elizabeth
` Rainbeau†, Paul J. Reider†, Karen Rex§, Aaron Siegmund†, Yaxiong Sun‡, Andrew S. Tasker†,
` Ning Xi†, Shimin Xu†, Yajing Yang§, Yihong Zhang§, Teresa L. Burgess§, Isabelle Dussault§
` and Tae-Seong Kim
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`175. “An Integrated High-Throughput Screening Approach for Purification of Solid Organic Compounds
`by Trituration and Crystallization in Solvents”, Organic Process Research & Development (2008),
`12, 58–65, Helming Tan,* Maggie Reed, Kyung H. Gahm, Tony King, Mina Dilmeghani Seran,
`Tracy Bostick, Van Luu, David Semin, Janet Cheetham, Rob Larsen, Mike Martinelli, and Paul
`Reider
`“Identification of a Nonpeptidic and Conformationally Restricted Bradykinin B1 Receptor
`Antagonist with Anti-Inflammatory Activity”, J. Med. Chem, (2007), 50, 607-610, D. D’Amico, T.
`Aya, J. Human, C. Fotsch, J.J. Chen, K. Biswas, B. Riahi, M.H. Norman, C.A. Willoughby, R.
`Hungate, P.J. Reider, G. Biddlecome, D Lester-Zeiner, C. Van Staden, E. Johnson, A. Kamassah, L.
`Arik, J. Wang, V.N. Viswanadhan, R.D. Groneberg, J. Zhan, H. Sizuke, A. Toro, D.A. Mareska,
`D.E. Clarke, D.M. Harvey, L.E. Burgess, E.R. Laird, B. Askew, G. Ng
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`173. “New Air-Stable Catalysts for General and Efficient Suzuki-Miyaura Cross-Coupling Reactions of
`Heteroaryl Chlorides”, Organic Letters, (2006), 8,9, 1787-1789, A.S. Guram, A.O. King, J.G. Allen,
`X. Wang, L.B. Schenkel, J. Chan, E.E. Bunel, M.M. Faul, R.D. Larsen, M.J. Martinelli, P.J. Reider
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`172. A Practical Synthesis of 2-((Pyrrolo[2,3-b]pyridine-4yl)methylamino)-5-fluoronicotinic Acid, J.
`Org. Chem, 2006, 71, 4021-4023, X Wang, B Zhi, J Baum, Y. Chen, R. Crockett, L. Huang, S.
`Eisenberg, J. Ng, R. Larsen, M. Martinelli, P.J. Reider
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`171. “Effect of Microwave Heating on Ullmann-Type Heterocycle-Aryl Ether Synthesis Using Chloro-
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`174.
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`Heterocycles”, Tetrahedron Letters, (2006), 47,29, 5045-5048, N.D. D’Angelo, J.J. Peterson, S.K.
`Booker, I. Fellows, C. Dominguez, R. Hungate, P.J. Reider, T-S. Kim
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`170. “A Highly Enantioselective Catalyst for Asymmetric Hydroformylation of [2.2.1]-Bicyclic Olefins”,
`Tetrahedron Letters, (2005), 46,45, 7831-7834, J. Huang, E. Bunel, A. Allgeier, J. Tedrow, T. Storz,
`J. Preston, T. Correll, D. Manley, T. Soukup, R. Jensen, P.J. Reider
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`169. “A Soluble Base for the Copper-Catalyzed Imidazole N-Arylations with Aryl Halides”, J. Org.
`Chem., 2005, 70, 10135-10138, L. Liu, M. Frohn, N. Xi, C. Dominguez, R. Hungate, P.J. Reider
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`168. “Synthesis of a Substance P Antagonist: An Efficient Synthesis of 5-Substituted-4-N,N-
`dimethylamino-1,2,3-triazoles”, Organic Process Research & Development, 2005, 9,4, 490-498, M.
`Journet, D. Cai, D.L. Hughes, J.J. Kowal, R.D. Larsen, P.J. Reider
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`167. “Regio-Controlled Synthesis of N-substituted Imidazoles”, Tetrahedron Letters, (2005), 46,43, 7315-
`7319, N. Xi, S. Xu, Y. Cheng, A.S. Tasker, R.W. Hungate, P.J. Reider
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`166. “An Efficient Synthesis of an αvβ3 Antagonist”, J. Org.Chem., 2004, 69, 1959-1966, N. Yasuda, Y.
`Hsiao, M.S. Jensen, N.R. Rivera, C. Yang, K.M. Wells, J. Yau, M. Palucki, L. Tan, P.G. Dormer,
`R.P. Volant, D.L. Hughes, P.J. Reider
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`165. “Efficient Synthesis of NK1 Receptor Antagonist Aprepitant Using a Crystallization-Induced
`Diastereoselective Transformation”, J. Am. Chem. Soc., 2003, 125, 2129-3135, K.M.J. Brands, J.F.
`Payack, J.D. Rosen, T.D. Nelson, A. Candelario, M.A. Huffman, M.M. Zhao, J. Li, B. Craig, Z.J.
`Song, D.M. Tschaen, K. Hansen, P.N. Devine, P.J. Pye, K. Rossen, P.G. Dormer, R.A. Reamer, C.J.
`Welch, D.J. Mathre, N.N. Tsou, J.M. McNamara, P.J. Reider
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`164. “Highly Regioselective Friedländer Annulations with Unmodified Ketones Employing Novel Amine
`Catalysts: Syntheses of 2-Substituted Quinolines, 1,8-Naphthyridines, and Related Heterocycles”, J.
`Org. Chem., 2003, 68, 467-477, P.G. Dormer, K.K. Eng, R.N. Farr, G.R. Humphrey, J.C.
`McWilliams, P.J. Reider, J.W. Sager, R.P. Volante
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`163. “A Practical Synthesis for the Core Structure of a Family of Selective Prostaglandin D2 Receptor
`Antagonists”, J. Org. Chem., 2003, 68, 2338-2342, K.R. Campos, M. Journet, D. Cai, J.J. Kowal, S.
`Lee, R.D. Larsen, P.J. Reider
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`162. “Novel synthesis of sulfones from α, α-dibromomethyl aromatics”, Tetrahedron Letters (2003), 44,
`1283-1286, Feng Xu, Kimberly Savary, J. Michael Williams, E.J.J. Grabowski, P.J. Reider.
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`161. “Practical Routes to the Triarylsulfonyl Chloride Intermediate of a ß3 Adrenergic Receptor Agonist”,
`Tetrahedron Letters (2003), 59,8, 1317-1325, N. Ikemoto, J Liu, K.M.J. Brands, J.M. McNamara
`and P.J. Reider
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`160. “Preparation of a Clinically Investigated Ras Farnesyl Transferase Inhibitor”, J of Heterocyclic
`Chemistry, (2003), 40, 229-241, P.E. Maligres, M.S. Waters, S.A. Weissman, J.C. McWilliams, S
`Lewis, J Cowen, R.A. Reamer, R.P. Volante, P.J. Reider, D Askin
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`159. “An Efficient Synthesis of a Doxorubicin-Peptide Conjugate”, Synlett (2003), 05, Y-J Shi, M
`Cameron, U.H. Dolling, D.R. Lieberman, J.E. Lynch, R.A.Reamer, M.A. Robbins, R.P. Volante, P.J.
`Reider
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`158. “A Stereoselective Aldol Reaction Via Diisopinocampheyl Boron-Enolate in Preparation of
`Chromane Carboxylate with Quaternary Carbon”, Tetrahedron Letters, (2003), 44,28, 5285-5288, F.
`Lang, D. Zewge, Z.J. Song, B. Mirlinda, P. Dormer, D. Tschaen, R.P. Volante, P.J. Reider
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`157. “Asymmetric Synthesis of Cyclic Hydroxy Ketones Derived from Enol Ethers via Sharpless
`Asymmetric Dihydroxylation. A Study in the Correlation of the Enol Ether Chain Length and
`Enantioselectivity.”, J. Org. Chem. (2003), 68, 8088, Benjamin F. Marcune, Sandor Karady, Paul J.
`Reider, Ross A. Miller, Mirlinda Biba, Lisa DiMichele, and Robert A. Reamer.
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`156. “Stereoselective Synthesis from a Process Research Perspective”, Drug Discovery Today, (2002)
`7,5, 303-314, M.C. Hillier, P.J. Reider
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`155. “Efficient One-Pot Synthesis of the 2-Aminocarbonylpyrrolidin-4-ylthio-Containing Side Chain of
`the New Broad-Spectrum Carbapenem Antibiotic Ertapenem”, 2002, J. Org. Chem., 67, 4771-4776,
`K.M.J. Brands, R.B. Jobson, K.M. Conrad, J.M. Williams, B. Pipik, M. Cameron, A.J. Davies, P.G.
`Houghton, M.S. Ashwood, I.F. Cottrell, R.A. Reamer, D.J. Kennedy, U-H. Dolling, P.J. Reider
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`154. “Solvent-Dependent Dynamic Kinetic Asymmetric Transformation/Kinetic Resolution in
`Molybdenum-catalyzed Asymmetric Allylic Alkylations”, 2002, J. Org. Chem., 67, 2762-2768, D.L.
`Hughes, M. Palucki, N. Yasuda, R.A. Reamer, P.J. Reider
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`153. “Development of a New and Practical Route to Chiral 3,4-Disubstituted Cyclopentanones:
`Asymmetric Alkylation and Intramolecular Cyclopropanation as Key C-C Bond-Forming Steps”,
`2002, J. Org. Chem., 67, 5508-5516, M. Palucki, J.M. Um, N. Yasuda, D.A. Conlon, F-R Tsay, F.W.
`Hartner, Y. Hsiao, B Marcune, S. Karady, D.L. Hughes, P.G. Dormer, P.J. Reider
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`152. “Efficient Synthesis of 6-mono-bromo-1,1’-bi-2naphthol”, Tetrahedron Letters (2002), 43,22, 4055-
`4057, D Cai, R.D. Larsen, P.J. Reider.
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`151. “Practical Enantioselective Synthesis of a COX-2 Specific Inhibitor”, Tetrahedron Letters, (2002),
`58,37, 7403-7410, L Tan, C-Y Chen, W Chen, L Frey, A.O. King, R.D. Tillyer, F Xu, D Zhao, E.J.J.
`Grabowski, P.J. Reider, et al.
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`150. “Aza-Diels-Alder/intramolecular Heck Cyclization Approach to the Tetrahydro-ß-Carboline
`Skeleton of the Ajmaline/Sarpagine Alkaloids”, Tetrahedron Letters (2002), 43,21, 3871-3874, J.T.
`Kuethe, A. Wong, I.W. Davies, P.J. Reider
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`149. “Asymmetric Aza-Diels-Alder Reactions of Indole 2-carboxaldehydes”, Tetrahedron Letters (2002),
`43,1, 29-32, J.T. Kuethe, I.W. Davies, P.G. Dormer, R.A. Reamer, D.J. Mathre, P.J. Reider
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`148. “Practical Asymmetric Synthesis of Aprepitant, a Potent Human NK-1 Receptor Antagonist, via a
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`Stereoselective Lewis Acid-Catalyzed Trans Acetalization Reaction, J. Org. Chem. (2002), 67,
`6743-6747, M.M. Zhao, J.M. McNamara, G-J Ho, K.M. Emerson, Z.J. Song, D.M. Tschaen, K.M.J.
`Brands, U-H. Dolling, E J.J. Grabowski, P.J. Reider.
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`147. “A general method for the highly diastereoselective, kinetically controlled alkylation of (+)-
`nopinone”, Tetrahedron Letters (2002), 43, 6957-6959, K.R. Campos, S. Lee, M. Journet, J.J.
`Kowal, D. Cai, R.D. Larsen, P.J. Reider.
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`146. “Effective Lithiation of 3-Bromopyridine: Synthesis of 3-Pyridine Boronic Acid and Varioustly 3-
`Substituted Pyridines”, Tetrahedron Letters (2002), 43, 4285, D. Cai, R.D. Larsen, P.J. Reider.
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`145. “Efficient Synthesis of the Optically Active Dihydropyrimidinone of a Potent a1A-Selective
`Adrenoceptor Antagonist”, Can J. Chem (2002), 80, 646, D.R. Sidler, N Barta, W Li, E Hu, L mtty,
`N. Ikemoto, J.S. Campbell, M. Chartrain, K. Gbewonyo, R. Boyd, E.G., Corley, R.G. Ball, R.D.
`Larsen, P.J. Reider.
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`144. “Asymmetric Synthesis of 1,2,3-Trisubstituted Cyclopentanes and Cyclohexanes as Key
`Compenents of Substance P Antagonists, J. Org. Chem. (2002), 67, 5993-6000, J.T. Kuethe, A.
`Wong, J Wu, I.W. Davies, P.G. Dormer, C.J. Welch, M.C. Hillier, D.L. Hughes, P.J. Reider.
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`143. “Experimental and Theoretical Studies on the Oxidative Addition of Palladium(0) to ß-
`chlorovinamidinium salts”, Tetrahedron Letters, (2001), 57,24, 5061-5066, I.W. Davies, J Wu, J-F
`Marcoux, M Taylor, D Hughes, P.J. Reider and R.J. Deeth
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`142. “Asymmetric Synthesis of cis-aminochromanol”, Tetrahedron Letters, (2001), 42,50, 8743-8745,
`K.B. Hansen, P. Rabbat, S.A. Springfield, P.N. Devine, E.J.J. Grabowski, P.J. Reider
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`141. “Radical Alkylation of N-alkyl 1,2,4-triazoles”, Tetrahedron Letters, (2001), 42,42, 7353-7355, K.B.
`Hansen, P.Rabbat, S.A. Springfield, R. Desmond, P.N. Devine, E.J.J. Grabowski, P.J. Reider
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`140. “Asymmetric Synthesis of (2S,3S)-3-hydroxy-2-phenylpiperidine Via Ring Expansion”, Tetrahedron
`Letters, (2001), 42,36, 6223-6225, J. Lee, T. Hoang, S. Lewis, S.S. Weissman, D. Askin, R.P.
`Volante, P.J. Reider
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`139. “A Highly Efficient Synthesis of 2-[3-aminopropyl]-5,6,7,8-tetrahydronaphthyridine via a Double
`Suzuki Reaction and a Chichibabin Cyclization”, Tetrahedron Letters (2001), 42, 6811, M. Palucki,
`D.L. Hughes, N. Yasuda, C. Yang, P.J. Reider.
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`138. “Practical Routes Toward the Synthesis of 2-halo- and 2-alkylamino-4-pyridine-carboxaldehydes”,
`Tetrahedron Letters (2001), 42, 6815, L.F. Frey, K. Marcantonio, D.E. Frantz, J.A. Murry, R.D.
`Tillyer, E.J.J. Grabowski, P.J. Reider.
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`137. “A General Preparation of Pyridines and Pyridones via the Annulation of Ketones and Esters”, J.
`Org. Chem. (2001), 66(12), 4194-4199, J-F. Marcoux, F-A. Marcotte, J. Wu, P. Dormer, I.W.
`Davies, D. Hughes, P.J. Reider.
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`136. “Controlled Semihydrogenation of Aminoalkynes Using Ethylenediamine as a Poison of Lindlar’s
`Catalyst”, J. Org. Chem. (2001), 66(10), 3634-3635, K.R. Campos, D. Cai, M. Journet, J.J. Kowal,
`R.D. Larsen, P.J. Reider.
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`135. “Highly Regioselective Friedlaender Reaction”, Org. Lett. (2001), 3(8), 1101-1103, Y. Hsiao, N.R.
`Rivera, N. Yasuda, D.L. Hughes, P.J. Reider.
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`134. “Molybdenum-catalyzed Asymmetric Allylic Alkylation Reactions Using Mo(CO)6 asPrecatalyst”,
`Adv. Synth. Catal. (2001), 343(1), 46-50, M. Palucki, J.M. Um, D.A. Conlon. N. Yasuda, D.L.
`Hughes, B. Mao, J. Wang, P.J. Reider.
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`133. “A Double Ring Closing Metathesis Reaction in the Rapid, Enantioselective Synthesis of NK-1
`Receptor Antagonists”, Org Lett. (2001), 3(5), 671-674, D.J. Wallace, J.M. Goodman, D.J. Kennedy,
`A.J. Davies, C.J. Cowden, M.S. Ashwood, I.F. Cottrell, U.H. Dolling, P.J. Reider.
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`132. “Asymmetric Bioreductions: Application to the Synthesis of Pharmaceuticals”, J. Mol., Catal. B:
`Enzym. (2001), 11(4-6), 503-512, M. Chartrain, R. Greasham, J. Moore, P.J. Reider, D. Robinson,
`B. Buckland.
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`131. “.beta.-Regioselective Intermolecular Heck Arylation of N,N-disubstituted Allylamines”,
`Tetrahedron Lett. (2001), s42(2), 159-162, J. Wu, J-F. Marcoux, I.W. Davies, P.J. Reider.
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`130. “A General [3 + 2 + 1] Annulation Strategy for the Preparation of Pyridine N-oxides”, Org. Lett.
`(2001), 3(2), 209-211, I.W. Davies, J-F. Marcoux, P.J. Reider.
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`129. “Preparation and Novel Reduction Reactions of Vinamidinium Salts”, J. Org. Chem. (2001), 66(1),
`251-255, I.W. Davies, M. Taylor, J-F. Marcoux, J. Wu, P.G. Dormer, D. Hughes, P.J. Reider.
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`128. “Improved Method for Rapid Evaluation of Chiral Stationary Phase Libraries”, Org. Lett. (2001),
`3(1), 95-98, C.J. Welch, S.D. Pollard, D.J. Mathre, P.J. Reider.
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`127. “Stereoselective Hydrogen Bromide-promoted Hydrogenation of an .alpha.-hydroxy Oxime”,
`Tetrahedron Lett. (2000), 41(42), 8021-8025, I.W. Davies, M. Taylor, J-F. Marcoux, L. Matty, J.
`Wu, D. Hughes, P.J. Reider.
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`126. “Highly Enantioselective 1,2-Addition of Lithium Acetylide –Ephedrate Complexes: Spectroscopic
`Evidence for Reaction Proceeding via a 2:2 Tetramer, and X-ray Characterization of Related
`Complexes”, J. Am. Chem. Soc. (2000), 122(45), 11212-11218, F. Xu, R.A. Reamer, R. Tillyer,
`J.M. Cummins, E.J.J. Grabowski, D.B. Collum, J.C. Huffman, P.J. Reider.
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`125. “A Practical Synthesis of a COX-2-Specific Inhibitor”, J. Org. Chem. (2000), 65(25), 8415-8420,
`I.W. Davies, J-F. Marcoux, E.G. Corley, M. Journet, D-W. Cai, M. Palucki, J. Wu, R.D. Larsen, K.
`Rossen, P.J. Pye, L. DiMichele, P. Dormer, P.J. Reider.
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`124. “Hydrogen Iodide-Promoted Reduction of .beta.-Chlorovinamidinium Salts”, Org. Lett. (2000),
`2(21), 3385-3387, I.W. Davies, M. Taylor, D. Hughes, P.J. Reider
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`123. “Practical Modifications and Applications of the Sharpless Asymmetric Aminohydroxy-lation in the
`One-Pot Preparation of Chiral Oxazolidine-2-Ones”, Org. Lett. (2000), 2(18) 2821-2824, N.S. Barta,
`D.R. Sidler, K.B. Somerville, S.A. Weissman, R.D. Larsen, P.J. Reider.
`
`122. “Highly Asymmetric Dihydroxylation of 1-aryl-1’-pyridyl alkenes”, Tetrahedron Lett. (2000),
`41(25), 4865-4869, X. Wang, M. Zak, M. Maddess, P. O’Shea, R. Tillyer, E.J.J. Grabowski, P.J.
`Reider.
`
`121. “Annulation of Ketones with Vinamidinium Hexafluorophosphate Salts: An Efficient Preparation of
`Trisubstituted Pyridines”, Org. Lett. (2000), 2(15), 2339-2341, J-F. Marcoux, E.G. Corley, K.
`Rossen, P. Pye, J. Wu, M.A. Robbins, I.W. Davies, R.D. Larsen, P.J. Reider.
`
`120. “Selective Monolithiation of 2,5-dibromopyridine with butyllithium”, Tetrahedron Lett, (2000),
`41(22), 4335-4338, X. Wang, P. Rabbat, P. O’Shea, R. Tillyer, E.J.J. Grabowski, P.J. Reider.
`
`119. “An Efficient Preparation of Vinamidinium Hexafluorophosphate Salts”, J. Org. Chem. (2000),
`65(15), 4571-4574, I.W. Davies, J-F. Marcoux, J. Wu, M. Palucki, E.G. Corley, M.A. Robbins, N.
`Tsou, R.G. Ball, P. Dormer, R.D. Larsen, P.J. Reider.
`
`118. “Rhodium-carbenoid-mediated Intermolecular O-H Insertion Reactions: A Dramatic Additive
`Effect. Application in the Synthesis of an Ascomycin Derivative”, Tetrahedron Lett. (2000), 41(12),
`1877-1881, T. Nelson, Z.J. Song, A.S. Thompson, M. Zhao, DeMarco, R.A. Reamer, M.F.
`Huntington, E.J.J. Grabowski, P.J. Reider.
`
`117. “Synthesis of an Anti-Methicillin-Resistant Staphylococcus Aureus (MRSA) Carbapenem via
`Stannatrane-Mediated Stille Coupling”, Org. Lett. (2000), 2(8), 1081-1084, M.S. Jensen, Yang, Y.
`Hsiao, N. Rivera, K.M. Wells, J.Y. Chung, N. Yasuda, D.L. Hughes, P.J. Reider
`
`116. “A Practical and Efficient Preparation of the Releasable Naphthosultam Side Chain of a Novel Anti-
`MRSA Carbapenem”, J. Org. Chem. (2000), 65(5), 1399-1406, R.A. Miller, G.R. Humphrey, D.R.
`Lieberman, S.S. Ceglia, D.J. Kennedy, E.J.J. Grabowski, P.J. Reider.
`
`115. “Rapid Assembly of Substituted Dihydrocyclohepta[3,4]pyrrolo[1,2-a]indoles via Novel, Carbene-
`Based, Rearrangement Reaction, J. Am. Chem. Soc. (2000), 122(6), 1215-1216, L.F. Frey, R.D.
`Tillyer, S.G. Ouellet, R.A. Reamer, E.J.J. Grabowski, P.J. Reider.
`
`114. “Bioreactor Systems in Drug Metabolism: Synthesis of Cytochrome P450-Generated Metabolites”,
`Metabolic Engineering (2000), 115-125, T.H. Rushmore, P.J. Reider, D. Slaughter, C. Assang, M.
`Shou.
`
`113. “Practical Asymmetric Synthesis of an Endothelin Receptor Antagonist”, J. Org. Chem. (1999),
`64(26), 9658-9667, Z.J. Song, M. Zhao, R. Desmond, P. Devine, D.M. Tschaen, R. Tillyer, L. Frey,
`R. Heid, F. Xu, B. Foster, J. Li, R. Reamer, R. Volante, E.J.J. Grabowski U.H. Dolling, S. Okada, Y.
`Kato, E. Mano, P.J. Reider.
`
`
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`8
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`112. “Efficient and Practical Synthesis of a Potent anti-MRSA.beta.-Methylcarbapenem Containing a
`Releasable Side Chain”, J. Am. Chem. Soc. (1999), 121(49), 11261-11266, G.R. Humphrey, R.A.
`Miller, P.J. Pye, K. Rossen, R.A. Reamer, A. Maliakal, S.S. Ceglia, E.J.J. Grabowski, R.P. Volante,
`P.J. Reider.
`
`111. “Sequential Nitromethane Conjugate Addition/Elimination-Pd-Catalyzed Allylation of .beta.-
`Trifloxy Acrylates. Application to Carbapenem Synthesis”, Org. Lett. (1999), 1(11), 1783-1785,
`J.Y.L. Chung, E.J.J. Grabowski, P.J. Reider.
`
`110. “A highly Convergent Synthesis of a Fibrinogen Receptor Antagonist”, J. Org. Chem. (1999),
`64(21), 7751-7755, F.W. Hartner, R.J. Cvetovich, F-R. Tsay, J.S. Amato, B. Pipik, E.J.J. Grabowski,
`P.J. Reider.
`
`109. “Practical Chemoenzymatic Synthesis of a 3-pyridylethanolamino.beta.3 adrenergic receptor
`Agonist”, Tetrahedron Lett. (1999), 40(37), 6739-6743, J.Y.L. Chung, G-J, Ho, M. Chatrain,
`Roberge, D. Zhao, J. Leazer, R. Farr, M. Robbins, K. Emerson, D.J. Mathre, J.M. McNamara, D.L.
`Hughes, E.J.J. Grabowski, P.J. Reider.
`
`108. “Enantioselective Alkynylation of Aromatic Aldehydes Catalyzed by Readily Available Chiral
`Amino Alcohol-Based Ligands”, Synthesis (1999), (Spec. Iss.), 1453-1458, Z. Li, V. Upadhyay,
`A.E. DeCamp, L. DiMichele, P.J. Reider.
`
`107. “(1S,2R)-1-aminoindan-2-ol (1H-inden-2-ol, 1-amino-2,3-dihydro-(1S-cis)-)”, Org. Synth. (1999),
`76, 46-56, J.F. Larrow, E. Roberts, T.R. Verhoeven, K.M. Ryan, C.H. Senanayake, E.N. Jacobsen,
`P.J. Reider.
`
`106. “(R )-(+)- and (S)-(-)-2,2’-bis(diphenylphosphino)-1,1’binaphyl (BINAP) (phosphine,
`[1,1’binaphthalene]-2,2’diylbis[diphenyl-, (R ) and (S))”, Org. Synth. (1999), 76, 6-11, D. Cai, J.F.
`Payack, D.R. Bender, D.L. Hughes, T.R. Verhoeven, P.J. Reider.
`
`105. “Synthesis of benzofuroquinolizine for .alapha.-2 adrenoceptor antagonsit MK-912: an O-analogue
`of the Pictet-Spengler reaction”, Tetrahedron Lett. (1999), 40(27), 4917-4920, J. Albaneze-Walker,
`K. Rossen, R.A. Reamer, R.P. Volante, P.J. Reider.
`
`104. “Resolution of 1,1’-bi-2-naphtol (1,1’-binaphthalene]-2,2’-diol), Org. Synth. (1999), 76, 1-5, Cai,
`D.L. Hughes, T.R. Verhoeven, P.J. Reider.
`
`103. “Metabolic Interactions Between Mibefradil and HMG-CoA Reductase Inhibitors: An In Vitro
`Investigation with Human Liver Preparations”, Br. J. Clin. Pharmacol. (1999), 47(3), 291-298, T.
`Prueksaritanont, M. Bennett, C. Tang, Y. Meng, C. Assang, P. Lu, J.H. Lin, T.A. Baillie, P.J. Reider.
`
`102. “Efficient Syntheses of 2-(3’,5’-difluorophenyl)-3-(4’-methylsulfonylphenyl)cyclopent-2-enone, a
`potent COX-2 inhibitor”, Tetrahedron (1999), 55(19), 6001-6018, D. Zhao, F. Xu, C-Y. Chen, R.D.
`Tillyer, E.J.J. Grabowski, P.J. Reider, C Black, N Ouimet and P Prasit
`
`101. “A Chemical Synthesis of Nicotinamide Adenine Dinucleotide (NAD+), Chem. Commun,
`
`
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`9
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`
`
`
`
`
`100.
`
` 95.
`
` 94.
`
` 93.
`
`(Cambridge) (1999), (8), 729-730, J. Lee, H. Churchill, W-B. Choi, J.E. Lynch, F.E. Roberts R.P.
`Volante, P.J. Reider.
`
`“A Novel, Highly Enantioselective Ketone Alkynylation Reaction Mediated by Chiral Zinc
`Aminoalkoxides”, Angew. Chem., Int. Ed. (1999), 38(5), 711-713, L. Tan, C-Y. Chen, R.D. Tillyer,
`E.J.J. Grabowski, P.J. Reider.
`
` 99. “Semisynthesis of an Antifungal Lipopeptide Echinocandin”, J. Org. Chem. (1999), 64(7), 2411-
`2417, M. Journet, D. Cai, L.M. DiMichele, D.L. Hughes, R.D. Larsen, T.R. Verhoeven P.J. Reider.
`
` 98. “Oxidation of Primary alcohols to Carboxylic Acids with Sodium Chlorite Catalyzed by TEMPO
`and Bleach”, J. Org. Chem. (1999), 64(7), 2564-2566, M. Zhao, J. Li, E. Mano, Z. Song, D.M.
`Tschaen, E.J.J. Grabowski, P.J. Reider.
`
` 97. “Highly Chemoselective Trichloroacetimidate-Mediated Alkylation of Ascomycin: A Convergent,
`Practical Synthesis of the Imunosuppressant L-733,725, J. Org. Chem. (1999), 64(6), 1859-1867, Z.
`Song, A. DeMarco, M. Zhao, E.G. Corley, A.S. Thompson, J. McNamara, Y. Li, D. Rieger, P.
`Sohar, D.J. Mathre, D.M. Tschaen, R.A. Reamer, M.F. Huntington, G-J. Ho, F-R. Tsay, K. Emerson,
`R. Shuman, E.J.J. Grabowski, P.J. Reider.
`
` 96. “A CLFSE/MM study on the Role of Ligand Bite-Angle in Cu(II)-Catalyzed Diels-Alder
`Reactions”, Tetrahedron Lett. (1999), 40(7), 1233-1236, I.W. Davies, R.J. Deeth, R.D. Larsen, P.J.
`Reider.
`
`“Crystallization-induced Asymmetric Transformation: Stereospecific Synthesis of L-768,673,
`Tetrahedron (1999), 55(4), 909-918, Y-J. Shi, K.M. Wells, P.J. Pye, W-B. Choi, H.R.O. Churchill,
`J.E. Lynch, A. Maliakal, J.W. Sager, K.Rossen, R.P. Volante, P.J. Reider
`
`“Improved Stereoselectivity in the Heterogeneous Catalytic Synthesis of Enalapril Obtained
`Through Multidimensional Screening”, Tetrahedron Lett. (1999), 40(5), 831-834, M. Huffman, P.J.
`Reider.
`
`“Enantioselective alkynylation of Aromatic Aldehydes Catalyzed by Readily Available Chiral
`Amino Alcohol-Based Ligands", Synthesis (1999), 1453-1458, Z. Li, V. Upadhyay, A. DeCamp, L.
`DiMichele, P.J. Reider.
`
`“Enantioselective 1,4-addition of aryllithium reagents to α,β-unsaturated tert-butyl esters in the
`presence of chiral additives”, 1998, Tetrahedron: Asymmetry, 9,10, 1651-1655, F. Xu, R.D. Tillyer,
`D.M. Tschaen, E.J.J. Grabowski, P.J. Reider
`
`“[2.2]PHANEPHOS-Ruthenium(II) Complexes: Highly active asymmetric catalysts for the
`hydrogenation of ß-ketoesters”, Tetrahedron Letters, (1998), 39/25, 4441-4444, P.J. Pye, K. Rossen,
`R.A. Reamer, R.P. Volante, P.J. Reider
`
`“An Efficient Asymmetric Synthesis of a Potent COX-2 Inhibitor L-784,512”, Tetrahedron Letters,
`(1998), 39,23, 3961-3964, L. Tan, C-y Chen, R.D. Larsen, T.R. Verhoeven, P.J. Reider
`
`92.
`
`91.
`
`90.
`
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`10
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`89.
`
`88.
`
`87.
`
`86.
`
`85.
`
` 84.
`
` 83.
`
`
`“A Highly Enantioselective Asymmetric Hydrogenation Route to ß-(2R,3S)-methyltryptophan”,
`Tetrahedron Letters, (1998), 39,21, 3455-3458, R.S. Hoerrner, D. Askin, R.P. Volante, P.J. Reider
`
`“An Improved and Practical Procedure for the Synthesis of Substituted Phenylacetylpyridines”,
`Tetrahedron Letters, (1998), 39,13, 1717-1720, M. Journet, C. Dongwei, R.D. Larsen, P.J. Reider
`
`“A Practical Preparation of Diisopropyl Phosphoryl Protected Amino Acids”, Tetrahedron Letters,
`(1998), 39,52, 9583-9586, K.M.J. Brands, K. Wiedbrauk, J.M. Williams, U.-H. Dolling, P.J.Reider
`
`“Efficient Synthesis of N-arylpiperazinones Via a Selective Intramolecular Mitsunobu
`Cyclodehydration”, Tetrahedron Letters, (1998), 39,41, 7459-7462, S.A. Weissman, S. Lewis, D.
`Askin, R.P. Volante, P.J. Reider
`
`“An Efficient Asymmetric Hydrogenation Approach to the Synthesis of the Crixivan® Piperazine
`Intermediate”, Tetrahedron Letters, (1998), 39,38, 6823-6826, K. Rossen, P.J. Pye, L.M. DiMichele,
`R.P. Volante, P.J. Reider
`
`“A Novel Chromium Trioxide Catalyzed Oxidation of Primary Alcohols to theCarboxylic Acids",
`Tetrahedron Letters (1998), 39 5323-5326, M. Zhao, J. Li, Z. Song, R. Desmond, D. Tschaen, E.J.J.
`Grabowski, P.J. Reider.
`
`“Ni-catalyzed Nucleophilic Conjugate Additions of Grignard and Organozincate Reagents to
`Substituted 4-Vinylpyridines. General Synthesis of Phosphodiesterase IV Inhibitors”. Tetrahedron,
`(1998), 54, 1185-1195, I.N. Houpis, J. Lee, I. Dorziotis, A. Molina R.A. Reamer, R.P. Volante and
`P.J. Reider.
`
`“Crystallization-Induced Asymmetric Transformation: Stereospecific Synthesis of L-768,673",
`Tetrahedron (1998), 909-918, Y-J. Shi, K. Wells, P. Pye, W-B. Choi, H. Churchill, J. Lynch, A.
`Maliakal, J. Sager, K. Rossen, R. Volante, P.J. Reider.
`
`“Practical Synthesis of Anti-Methicillin-Resistant Staphylococcus Aureus (MRSA) Carbapenem L-
`742,728", J. Org. Chem. (1998), 63, 5438-5446, N. Yasuda, M. Huffman G-J. Ho, L. Xavier, C.
`Yang, K. Emerson, F-R. Tsay, Y. Li, M. Kress, D. Rieger, S. Karady P. Sohar, N. Abramson, A.
`DeCamp, D. Mathre, A. Douglas, U-H. Dolling, E. Grabowski, P.J. Reider.
`
`“A Stereoselective Synthesis of a 2-functionalized-methyl-1β-methylcarbapenem
`KeyIntermediate via Decarboxylation, Chem. Commun. (1998), 1817-1818, W-B. Choi, J. Lee, J.
`Lynch, R. Volante, R. Reamer, P.J. Reider.
`
`“Practical Synthesis of α-Amino Acids Using CIS-Aminoindanol Derived Hippuric Acid Amide as a
`Glycine Enolate Equivalent”, Tetrahedron Letters, (1998), 39(22), 3679-3682, J. Lee, W-B. Choi, J.
`Lynch, R. Volante, P.J. Reider.
`
`78. “A Stereospecific Decarboxylation; a Key Reaction to an Intermediate for .beta.-Methyl-
`carbapenems”, Synth. Appl. Isot. Labelled Compd. 1997, W-B. Choi, H.R.O. Churchill, J.E. Lynch,
`
`82.
`
`81.
`
`80.
`
`79.
`
`
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`
`
`77.
`
` 76.
`
` 74.
`
` 72.
`
` 71.
`
`A.S. Thompson, G.R. Humphrey, R.P. Volante, I. Shinkai, P.J. Reider.
`
`“Nickel Catalyzed Addition of Organozincates to Optically Pure Vinylic Sulfoxides. Synthesis of
`the Phosphodiesterase IV Inhibitor L-765,527 (CDP-840)”, Tetrahedron Letters, (1997), 38,41,
`7131-7134, I.N. Houpis, A. Molina, I. Dorziotis, R.A. Reamer, R.P. Volante, P.J. Reider
`
`“A Convenient and Economical Method for the Preparation of DIP-Chloride™ and Its Application
`in the Asymmetric Reduction of Aralkyl Ketones”, Tetrahedron Letters (1997), 38(15), 2641-2644.
`M. Zhao, A.O. King, R.D. Larsen, T.R. Verhoeven, P.J. Reider.
`
` 75. “A Stereospecific Decarboxylation; a Key Reaction to an Intermediate for Β-Methylcarba-penems,
`"W.-B. Choi, H.R.O. Churchill, J.E. Lynch, A.S. Thompson, G.R. Humphrey, R.P. Volante, P.J.
`Reider, I. Shinkai, D.K. Jones and D.C. Liotta, Synthesis and Applications of Isotopically Labelled
`Compounds Proceedings of the Sixth International Symposium, Phil. PA 14-18 September 1997, Ed.
`J.R. Heys and D.G. Melillo, John Wiley and Sons, London 1998.
`
`“Advances in AIDS Chemotherapy: The Asymmetric Synthesis of CRIXIVANTM”. Chimia 51
`(1997), 306, P.J. Reider.
`
` 73. “Synthesis of the Orally Active Spiroindoline-Based Growth Hormone Secretagogue, MK-677”.
`Tetrahedron, (1997), 53(32), 10983-10992. P.E. Maligres, I. Houpis, Rossen, A. Molina, J. Sager,
`V. Upadhyay, K.M. Wells, R.A. Reamer, J.E. Lynch, Askin, R.P. Volante, P. Houghton and
`P.J. Reider.
`
`“Nosylaziridines: Activated Aziridine Electrophiles”. Tetrahedron Letters, (1997), 38(30), 5253-
`5256. P.E. Maligres, M.M. See, D. Askin and P.J. Reid