`
`CURRICULUM VITAE
`Robert Michael Williams, Ph.D.
`University Distinguished Professor of Chemistry
`Department of Chemistry, Colorado State University, Fort Collins, CO 80523
`Phone (970) 491-6747; FAX (970)-491-3944
`e-mail: robert.williams@colostate.edu
`Webpage: http://rwindigo1.chm.colostate.edu/
` Personal Information:
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`Date of birth: February 8, 1953
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`Married: Jill Janssen Williams
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`Children: Ridge Janssen Williams (born February 23, 2001)
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` Rainier Valentine Williams (born August 20, 2005)
`Education:
`B.A., Chemistry (with highest distinction), May, 1975. Syracuse University, Syracuse,
`NY. Thesis under Professor Ei-ichi Negishi on "A Stereoselective Synthesis of
`Partially Substituted 1,2,3-Butatriene Derivatives via Hydroboration".
`Ph.D., Organic Chemistry, June, 1979. Massachusetts Institute of Technology, Cambridge, MA. Thesis
`advisor, Dr. W. H. Rastetter. Thesis title: "Epidithiapiperazinedione Syntheses".
`Postdoctoral Fellow, September 1979-September 1980, Harvard University, Cambridge, MA. The late
`Professor R. B. Woodward group (Y. Kishi, principal investigator). Total synthesis of erythromycin A.
`Honors and Awards:
`Organic Synthesis Award, Local Rocky Mountain ACS Section, Reaching New Heights (2012)
`JSPS Invitation Fellowship Program for Research in Japan (Long-Term) 2012-2013
`Ernest Guenther Award in the Chemistry of Natural Products, American Chemical Society (2011)
`Multiple Myeloma Research Foundation Senior Award (2009-2011)
`University Distinguished Professor, Colorado State University (2002)
`Arthur C. Cope Scholar Award, American Chemical Society (2002)
`Japanese Society for the Promotion of Science (JSPS) Fellowship (1999)
`Merck & Co. Academic Development Award (1991-93)
`Fellow of the Alfred P. Sloan Foundation (1986-88)
`Eli Lilly Young Investigator Grantee (1986-88)
`NIH Research Career Development Awardee (1984-89)
`Phi Beta Kappa, Syracuse University (1975)
`Kanner Prize for Chemistry and Physics, Syracuse University (1974)
`Research and Professional Experience:
`Director, Colorado Center for Drug Discovery (C2D2), April 2012 -present
`Co-Director, Infectious Diseases Supercluster in Developmental Therapeutics at CSU
`Co-Director, Cancer Supercluster in Developmental Therapeutics at CSU
`Member, University of Colorado Cancer Center 2004-present
`University Distinguished Professor, Colorado State University 2002-present
`Professor, Colorado State University; Fort Collins, Colorado, January 1988-2002
`Associate Professor, Colorado State University; Fort Collins, Colorado, July 1985-December 1987
`Assistant Professor, Colorado State University; Fort Collins, Colorado, September 1980-June 1985
`Visiting Professor, University of California, Berkeley, CA September 1990-December 1990
`Visiting Professor of Chemistry, Harvard University, Cambridge, Mass. Sept. 15, 1994-Feb. 15, 1995
`Professional Society Memberships:
`American Association for the Advancement of Science
`American Chemical Society
`Japan Antibiotics Research Association
`International Society of Heterocyclic Chemistry
`Phi Beta Kappa
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`Editorial:
`(1) Associate Editor, Tetrahedron: Asymmetry (2006-2008)
`(2) Member, Editorial Board "Chemistry and Biology" Current Biology, Ltd. (1994-present).
`(3) Member, Editorial Advisory Board for Mini-Reviews in Organic Chemistry, Bentham Science Pubs.
`(2004-2012).
`(4) Co-Editor for the “Organic Chemistry Series”, Elsevier (Sir J.E. Baldwin co-Ed.) 1997-2012.
`(5) Editor-in-Chief for "Amino Acids", Springer-Verlag (1991-1998).
`(6) Acting Associate Editor for the Journal of the American Chemical Society; Sept. 1983-Jan. 1984.
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`Consulting Activities:
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`Cetya Therapeutics, Fort Collins, Colorado (2012-present)
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`Sapientia Therapeutics, Philadelphia, Pennsylvania (2012-present)
`Arch Therapeutics, Cambridge, Massachusetts (2010-present)
`HemaQuest Pharmaceuticals, Boston, Massachusetts (2006-2014)
`Ajinomoto Co., Yokohama Japan (2002-2013)
`Xcyte Therapies, Inc., Seattle, Washington (1996-2006)
`NewBiotics, Inc., SanDiego, California (2001-2002)
`Cubist Pharmaceutical Co., Cambridge, Massachusetts (2000-2003)
`Microcide Pharmaceuticals, Mountainview, California (1993-1998)
`Boehringer Ingelheim Pharmaceuticals, Ridgefield, Connecticut (1992-1993)
`Hoffmann-La Roche, Inc., Nutley, New Jersey (1989-1992)
`EPIX Medical, Cambridge, Massachusetts (1993-1997)
`W.R. Grace Company, Columbia, Maryland (1985-1990)
`G.D. Searle Co., St. Louis, Missouri (1988-1990)
`Nutrasweet Co., Skokie, Illinois (1990-1991)
`Symphony Pharmaceutical Co., Philadelphia, Pennsylvania (1991-1993)
`Venture Capital Corporate Boards and Scientific Advisory Boards:
`(1) Founding Scientist, Acting President, Member of the Board of Directors and Member of the
`Scientific Advisory Board of Cetya Therapeutics, Fort Collins, Colorado 2012-present.
`(2) Founding Scientist and Member of the Scientific Advisory Board for Sapientia Therapeutics
`(2012-present).
`(3) Consultant and Member of the Scientific Advisory Board for Arch Therapeutics, Cambridge,
`Mass. 2010-present.
`(4) Founding Scientist, Acting Vice-President of Discovery Chemistry, consultant and Member of
`the Scientific Advisory Board of HemaQuest, Seattle, Washington. 2006-present.
`(5) Founding Scientist and Member of the Corporate Board of Directors for Xcyte Therapies,
`Seattle, Washington. 1996-2006.
`(6) Scientific Advisory Board Member of Xcyte Therapies, Seattle, Washington. 1996-2006.
`(7) Scientific Advisory Board Member of NewBiotics, Inc., San Diego, CA. 2001-2004.
`(8) Founding Scientist and Scientific Advisory Board Member for Microcide Pharmaceuticals,
`Inc., Mountainview, California 1993-1998.
`Advisory Boards:
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`Member of the Advisory Board of the Los Alamos Stable Isotope Resource (1999-2007)
`Member of the Advisory Board for the Puerto Rico Alliance for the Advancement of Biomedical
`Research Excellence (PRAABRE) (2006-present)
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`Teaching
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`Graduate
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`C651 - "Molecular Basis for Drug Action and Design: Mechanism-Based Enzyme Inhibitors"
`C651 - "Total Synthesis of Natural Products"
`C651 - “Biosynthesis of Primary and Secondary Metabolites”
`C541 - "Spectroscopic Methods"
`C545 - "Advanced Organic Synthesis I”
`C549 – “Advanced Organic Synthesis II”
`C-547 – “Chemical Biology”
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`Undergraduate
`C340H - “Honors Organic Chemistry I”
`C341 - "Organic Chemistry I"
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`C343 - "Organic Chemistry II"
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`C245 - "Organic and Biological Chemistry"
`C345 - "Organic Chemistry I"
`C346 – “Organic Chemistry II”
`Chem 17 (Harvard University, 1994 - 1995)
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`Ph.D. Theses Directed:
`Robert W. Armstrong
`(1984)
`Andrew O. Stewart
`(1987)
`Peter J. Sinclair
`(1987)
`Lynn K. Maruyama
`(1987)
`Paul P. Ehrlich
`(1989)
`Myeong-Nyeo Im
`(1991)
`James A. Hendrix
`(1992)
`Sean C. Esslinger
`(1993)
`Glenn J. Fegley
`(1993)
`Gregory F. Miknis
`(1993)
`Timothy D. Cushing
`(1993)
`Mark E. Flanagan
`(1995)
`Steve Rubenstein
`(1996)
`Jennifer Travers
`(1995)
`Samuel B. Rollins
`(1997)
`Scott R. Rajski
`(1997)
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`Chester Yuan
`Bradley Herberich
`Jeffrey Cao
`Kathleen M. Halligan
`Jack D. Scott
`Emily M. Stocking
`Paul R. Sebahar
`Ted C. Judd
`Steven R. Lenger
`Duane E. DeMong
`Brian K. Albrecht
`Ryan E. Looper
`Yuyin Chen
`Alan W. Grubbs
`Siyuan Chen
`Chandele Gray
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`Xiangna Jia
`(1997)
`(1999) Daniel A. Gubler
`(2000)
`Tenaya Newkirk
`(2000)
`Cameron Burnett
`(2001)
`Brandon J. English
`(2001)
`Jennifer M. Finefield
`(2003)
`Timmy McAfoos
`(2003) Ryan J. Rafferty
`(2003) Guojun Pan
`(2003)
`Paul T. Schuber
`(2003)
`Guojun Pan
`(2004)
`Timothy R. Welch
`(2006)
`Jennifer M. Guerra
`(2006)
`Aaron Pearson
`(2007)
`Alberto Jimenez
`(2008)
`Michelle Sanchez
`Vy Le
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`(2009)
`(2009)
`(2009)
`(2009)
`(2010)
`(2011)
`(2011)
`(2011)
`(2011)
`(2011)
`(2011)
`(2011)
`(2012)
`(2013)
`(2013)
`(2014)
`(2017)
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`Masters Theses Directed:
`Tracy N. Tippie
`(1995) Christie Kosogof
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`Paul B. Gansle
`(1997) Meriah W.N. Valente
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`David M. Bender
`(1998) Nick Gearhart
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`Reviewer for Journals:
`Journal of the American Chemical Society
`Chemical Society Reviews
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`Journal of Organic Chemistry
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`Canadian Journal of Chemistry]
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`Archives of Biochemistry and Biophysics
`Bioorganic and Medicinal Chemistry Letters
` Bioorganic and Medicinal Chemistry
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`Amino Acids
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`(2001) Annie Youngman
`(2006)
`Andrea Geiser
`(2008)
`Tatyana Sabodash
`Marie Trujillo
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`(2009)
`(2009)
`(2011)
`(2013)
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`Angewandte Chemie
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`Science
`Chemical Reviews
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`Tetrahedron
`Syn. Lett.
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`Tetrahedron Letters
`Synthesis Nature Protocols
`Organic Letters
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`Nature Chemistry
`Chemistry & Biology
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`Accounts of Chemical Research
`Chemical Communications
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`Reviewer for Proposals:
`National Institutes of Health Synthetic and Biological Chemistry B (SBCB) Study Section 2005
`National Institutes of Health Medicinal Chemistry Study Section (MCHA) (2002-2005)
`National Science Foundation
`National Institutes of Health Medicinal Chemistry Study Section (Feb. 1987)
`National Institutes of Health BNP Study Section (Feb. 1989)
`Research Corporation
`Petroleum Research Fund (ACS)
`State Board of Education, Idaho
`Ad-hoc reviewer for the Medicinal Chemistry Study Section (MCHA) February, 1987
`Ad-hoc reviewer for the Bioorganic and Natural Products Chemistry Study Section (BNP) Feb., 1990
`Member, NIH T-32 Chemistry / Biology Interface Training Grant Study Section, 1993
`Ad-hoc reviewer for the Medicinal Chemistry Study Section (MCHA) October, 1996
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`Committee Memberships (Colorado State University)
`Mis-conduct in Science Investigation Committee
`Council of Research Associate Deans
`University Distinguished Professors Selection Committee
`Colorado State University Patent Committee
`Graduate Operations Committee, Department of Chemistry
`Graduate Admissions Committee, Department of Chemistry
`Colorado State University Biosafety Committee
`Promotion and Tenure Committee, Department of Chemistry
`Executive Committee, Department of Chemistry
`Industrial Liaison Committee, Department of Chemistry
`Awards Committee, Department of Chemistry
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`Current Research Funding:
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`Active Grants (Robert M. Williams, PI: all projects)
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`(1)
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`08/01/14 – 07/31/19
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`2RO1 CA70375-13 (NIH/NCI)
`Title: “Total Synthesis and Biosynthesis of Bioactive Substances”
`$268,515 Annual Amount
`$1,292,938 Total Award
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`(2)
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`09/01/17 – 08/31/18
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`1R41HL136068-01
`Title: “Novel HDAC Inhibitors for Treatment of Hemoglobinopathies”
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`$241,742.00 Total Award
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`Chair, Organizer or Co-organizer of Scientific Meetings
`Robert M. Williams, Professor of Chemistry
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`(1) The 1987 NSF Workshop on Environmental Chemistry, Stanford Sierra Camp, Lake Tahoe,
`California, Sept. 25-27, 1987.
`(2) The 1989 Chemical Congress of Pacific Basin Societies, Honolulu, Hawaii, December 17-22, 1989.
`Co-organizer of a Symposium entitled: “Recent Developments in the Chemistry of Amino Acids”.
`(3) Special Bilateral U.S.-Britain Workshop entitled: "Asymmetric Synthesis" July 3-8, 1990. Pingree
`Park, Colorado. Co-organizer of this workshop.
`(4) NSF-JSPS Bilateral Seminar entitled: "Selectivity in Synthetic and Bio-Organic Chemistry", Tokyo,
`Japan, June 3-7, 1991. Co-organizer of this bilateral seminar.
`(5) The 3rd International Congress on Amino Acids, Vienna, Austria, August 23-27, 1993. Title:
`"Asymmetric Synthesis of Non-proteinogenic Amino Acids via Chiral Glycinates". Co-organizer of this
`meeting.
`(6) The John K. & Dolores Stille Symposium on “Biological Chemistry”, September 12, 1997. Organizer
`of this symposium.
`(7) The 60th Birthday Celebration for Professor Yoshito Kishi, Harvard University. April 13, 1997,
`Harvard University. Co-organizer of this symposium and reception.
`(8) The PacifiChem 2000 Conference, Honolulu, Hawaii, December 14-19, 2000. Organizer of a
`Symposium entitled: “Frontiers in Antibiotics: Synthesis, Design and Mode of Action”.
`(9) The 19th International Congress of Heterocyclic Chemistry, Fort Collins, Colorado. August, 2003.
`Vice-President, Chairman and Organizer of this meeting.
`(10) The PacifiChem 2005 Congress, Honolulu, Hawaii, December 15-20, 2005. Co-Chair, Symposium
`entitled: “Total Synthesis of Natural Products”
`(11) The 70th Birthday Celebration for Professor Yoshito Kishi, Harvard University. April 13, 2007,
`Harvard University. Co-organizer of this symposium and reception.
`(12) The Albert & Joan Meyers Symposium. October 24, 2008, Colorado State University. Co-organizer
`of this symposium and reception.
`(13) The PacifiChem 2010 Conference, Honolulu, Hawaii. Organizer of a Symposium entitled: “Natural
`Products Synthesis”
`(14) Robert Burns Woodward Memorial Symposium. National ACS Meeting in Boston, Massachusetts,
`August 22-26, 2010. Principal Co-organizer.
`(15) Robert Burns Woodward Centennial Symposium. National ACS Meeting in Washington, DC,
`August 21-25, 2017. Principal Co-organizer.
`(16) Symposium in Celebration of Professor Yoshito Kishi’s 80th Birth Year: Organic Synthesis Directed
`Toward Drug Discovery. Nagoya University, Nagoya, Japan, April 14, 2018. Principal Co-organizer.
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`Robert M. Williams
`Brief Biographical Sketch
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`Robert M. Williams was born in New York in 1953 and was raised in Huntington, Long Island by Edith and
`Valentine Williams. He attended Syracuse University from 1971-1975 and received the B.A. degree in Chemistry
`in 1975. While at Syracuse, he did undergraduate research with the recent Nobel Laureate, Prof. Ei-ichi Negishi in
`the area of hydroboration methodology. He then moved to Cambridge, Massachusetts and entered the Ph.D.
`program at MIT and obtained his Ph.D. degree in 1979 under the supervision of Prof. William H. Rastetter. His
`doctoral studies were concerned with the total synthesis of two fungal metabolites, gliovictin and hyalodendrin.
`Following completion of his doctoral studies, he joined the laboratories of the late Prof. R.B. Woodward in 1979
`whose postdoctoral group was subsequently managed by Professor Yoshito Kishi. His postdoctoral work was
`concerned with the completion of the total synthesis of erythromycin A. Upon completion of his postdoctoral
`tenure at Harvard, he joined the faculty at Colorado State University in 1980. He was promoted to Associate
`Professor with tenure in 1985, Full Professor in 1988, and University Distinguished Professor in 2002, his current
`position. Dr. Williams has received several Honors and Awards including the NIH Research Career Development
`Award (1984-1989); The Eli Lilly Young Investigator Award (1986); Fellow of the Alfred P. Sloan Foundation
`(1986); the Merck, Academic Development Award (1991), the Japanese Society for the Promotion of Science
`Fellowship (1999), the ACS Arthur C. Cope Scholars Award (2002), the ACS Ernest Guenther Award in the
`Chemistry of Natural Products (2011) and the Japanese Society for the Promotion of Science Long-term
`Fellowship (2012-2013). In 2002, he was named one of the twelve University Distinguished Professors, the
`highest honor and rank that Colorado State University bestows upon faculty. He spent a sabbatical at the
`University of California, Berkeley in 1990 in the laboratories of Professor Peter G. Schultz and was a visiting
`Professor at Harvard University in 1994 where he spent a sabbatical with Professor Stuart L. Schreiber and also
`taught Chem 17. He serves on the Editorial Board of the journal Chemistry & Biology and was an Editor for the
`journal Amino Acids (1991-1998). He has served as a Series co-Editor for The Organic Chemistry Series,
`published by Pergamon Press/Elsevier with Professor Sir Jack E. Baldwin of Oxford. Dr. Williams was a Scientific
`Founder and member of the Scientific Advisory Board of Microcide Pharmaceutical Co. from 1993-1998 located in
`Mountainview, California and was a Founding Scientist, Member of the Scientific Advisory Board and Member of
`the Board of Directors of Xcyte Therapies, located in Seattle, Washington from 1995-2006. Dr. Williams is
`currently a Scientific Founder, consultant, and member of the Scientific Advisory Board for HemaQuest
`Pharmaceuticals, located in Seattle, Washington from 2006-present and also serves as a consultant and Member
`of the Scientific Advisory Board for Arch Therapeutics, Cambridge, Mass. 2010-present. Dr. Williams is a
`Scientific Founder, Member of the Board of Directors, Chairman of the Scientific Advisory Board and acting
`President of Cetya Therapeutics, located in Fort Collins, Colorado. Dr. Williams is a Scientific Founder and
`Member of
`the Scientific Advisory Board of BriaCell/Sapientia Therapeutics,
`located
`in Philadelphia,
`Pennsylvania. Dr. Williams was named as Director for the Colorado Center for Drug Discovery (C2D2) in April,
`2012 and served in that capacity until 2016.
`Dr. Williams’ research results from the interplay of synthetic organic chemistry, microbiology, biochemistry
`and molecular biology. Dr. Williams research interests have included the total synthesis of natural products, the
`asymmetric synthesis of amino acids and peptide isosteres, studies on anti-tumor drug-DNA interactions, design
`and synthesis of antibiotics and DNA-cleaving molecules, combinatorial phage libraries and biosynthetic
`pathways. He has utilized natural products synthesis to probe and explore biomechanistic and biosynthetic
`problems with a particular emphasis on antitumor and antimicrobial antibiotics. He has developed technology for
`the asymmetric synthesis of a-amino acids and peptide isosteres that has been commercialized by Aldrich
`Chemical Co. and has written a monograph on this subject. Dr. Williams has extensive experience in Medicinal
`Chemistry, Process Chemistry and Pharmaceutical formulations.
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`Personal Interests: Downhill, cross-country, randonee and telemark skiing; rock electric & acoustic guitars;
`backpacking; mountain biking; running; bicycling; technical rock climbing; scuba diving; water skiing; surfing;
`sailing; photography; oil painting; oriental carpets; fine woodworking, furniture design and construction; golf;
`squash racquets; gardening; orchids; salt water aquarist.
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`PUBLICATIONS
`Robert M. Williams, Colorado State University
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`∫ A Stereoselective Synthesis of Partially Substituted 1,2,3-Butatriene Derivatives via
`Hydroboration, Yoshida, T.; Williams, R.M.; Negishi, E-i., J. Am. Chem. Soc., 1974, 96, 3688-
`3690.
`∫ A Stereoselective Synthesis of cis-Alkenylboranes, Negishi, E-i.; Williams, R.M.; Lew, G.;
`Yoshida, T., J. Organomet. Chem., 1975, 92, C4-C6.
`¶ An Efficient Synthesis of d,l-Gliovictin: Construction of the Hydroxymethyl Moiety via a 3-
`Formyl-2,5-Piperazinedione, Williams, R.M.; Rastetter, W.H., Tetrahedron Lett., 1979, 1187-
`1190.
`¶ Synthesis of the Fungal Metabolites (±)-Gliovictin and (±)-Hyalodendrin, Williams, R.M.;
`Rastetter, W.H., J. Org. Chem., 1980, 45, 2625-2631.
`§ Asymmetric Total Synthesis of Erythromycin I, Woodward, R.B.; Logusch, E.; Nambiar, K.P.;
`Sakan, K.; Ward, D.E.; Au-Yeung, B.W.; Balaram, P.; Browne, L.J.; Card, P.J.; Chen, C.H.;
`Chenevert, R.B.; Fliri, A.; Frobel, K.; Gais, H.J.; Garratt, D.G.; Hayakawa, K.; Heggie, W.;
`Hesson, D.P.; Hoppe, D.; Hoppe, I.; Hyatt, J.A.; Ikeda, D.; Jacobi, P.A.; Kim, K.S.; Kobuke, Y.;
`Kojima, K.; Krowicki, K.; Lee, V.J.; Leubert, T.; Malchenko, S.; Martens, J.; Mathews, R.S.; Ong,
`B.S.; Press, J.B.; RajanBabu, T.V.; Rousseau, G.; Sauter, H.M.; Suzuki, M.; Tatsuta, K.;
`Tolbert, L.M.; Truesdale, E.A.; Uchida, I.; Ueda, Y.; Uyehara, T.; Vasella, A.T.; Vladuchick,
`W.C.; Wade, P.A.; Williams, R.M.; Wong, H.N.-C. J. Am. Chem. Soc., 1981, 103, 3210-3213.
`§ Asymmetric Total Synthesis of Erythromycin II, Woodward, R.B.; Logusch, E.; Nambiar, K.P.;
`Sakan, K.; Ward, D.E.; Au-Yeung, B.W.; Balaram, P.; Browne, L.J.; Card, P.J.; Chen, C.H.;
`Chenevert, A.; Fliri, A.; Frobel, K.; Gais, H.J.; Garratt, D.G.; Hayakawa, K.; Heggie, W.; Hesson,
`D.P.; Hoppe, D.; Hoppe, I.; Hyatt, J.A.; Ikeda, D.; Jacobi, P.A.; Kim, K.S.; Kobuke, Y.; Kojima,
`K.; Krowicki, K.; Lee, V.J.; Leubert, T.; Malchenko, S.; Martens, J.; Mathews, R.S.; Ong, B.S.;
`Press, J.B.; RajanBabu, T.V.; Rousseau, G.; Sauter, H.M.; Suzuki, M.; Tatsuta, K.; Tolbert,
`L.M.; Truesdale, E.A.; Uchida, I.; Ueda, Y.; Uyehara, T.; Vasella, A.T.; Vladuchick, W.C.; Wade,
`P.A.; Williams, R.M.; Wong, H.N.-C., J. Am. Chem. Soc., 1981, 103, 3213-3215.
`§ Asymmetric Total Synthesis of Erythromycin III, Woodward, R.B.; Logusch, E.; Nambiar, K.P.;
`Sakan, K.; Ward, D.E.; Au-Yeung, B.W.; Balaram, P.; Browne, L.J.; Card, P.J.; Chen, C.H.;
`Chenevert, R.B.; Fliri, A.; Frobel, K.; Gais, H.J.; Garratt, D.G.; Hayakawa, K.; Heggie, W.;
`Hesson, D.P.; Hoppe, D.; Hoppe, I.; Hyatt, J.A.; Ikeda, D.; Jacobi, P.A.; Kim, K.S.; Kobuke, Y.;
`Kojima, K.; Krowicki, K.; Lee, V.J.; Leubert, T.; Malchenko, S.; Martens, J.; Mathews, R.S.; Ong,
`B.S.; Press, J.B.; RajanBabu, T.V.; Rousseau, G.; Sauter, H.M.; Suzuki, M.; Tatsuta, K.;
`Tolbert, L.M.; Truesdale, E.A.; Uchida, I.; Ueda, Y.; Uyehara, T.; Vasella, A.T.; Vladuchick,
`W.C.; Wade, P.A.; Williams, R.M.; Wong, H.N.-C., J. Am. Chem. Soc., 1981, 103, 3215-3217.
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` Syracuse University
`¶ MIT
`§ Harvard University
`*Colorado State University
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`1981
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`1982
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`1983
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`1984
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`1985
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`19.
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`20.
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`21.
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`1986
`22.
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`*Bicyclomycin Synthetic Studies: Utilization of Bridgehead Carbanions, Williams, R. M.,
`Tetrahedron Lett., 1981, 22, 2341-2344.
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`*A New and Efficient Cyclization Reaction to Construct the Bicyclomycin Ring System:
`Synthesis of N,N’-Dimethyl-4-des-methylene Bicyclomycin, Williams, R.M.; Anderson, O.P.;
`Armstrong, R.; Josey, J.; Meyers, H.; Eriksson, C., J. Am. Chem. Soc., 1982, 104, 6092-6099.
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`*C-Glycosidation of Pyridyl Thioglycosides. Williams, R.M.; Stewart, A.O., Tetrahedron Lett.,
`1983, 24, 2715-2718.
`*Regioselective Functionalization of Bicyclic Piperazinedione Bridgehead Carbanions. Williams,
`R.M.; Dung, J-S.; Josey, J.; Armstrong, R.W.; Meyers, H., J. Am. Chem. Soc., 1983, 105, 3214-
`3220.
`*Improved Synthesis and Absolute Configuration of (+)- and (-)-2,2,4-Trimethyl-1,3-dioxolane-4-
`carboxaldehyde. Dung, J-S.; Armstrong, R.W.; Anderson, O.P.; Williams, R.M., J. Org. Chem.,
`1983, 48, 3592-3594.
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`*Metal-Mediated Concomitant Silyl Ether Cleavage/Cyclization Reactions to Construct Bicyclic
`Piperazinediones and a New Polymer-Supported Hg(II) Perchlorate. Dung, J-S.; Armstrong,
`R.W.; Williams, R.M., J. Org. Chem., 1984, 49, 3416-3419.
`*Alternate Preparation of Methyl-3-amino-2,3,6-trideoxy-a-D-arabino-hexopyranoside and Chiral
`Intermediates for the Synthesis of Thienamycin. Stewart, A.O.; Williams, R.M., Carbohydrate
`Res., 1984, 135, 167-173.
`*Stereocontrolled Total Synthesis of (±)- and (+)-Bicyclomycin: New Carbon-Carbon Bond-
`Forming Reactions on Electrophilic Glycine Anhydride Derivatives. Williams, R.M.; Armstrong,
`R.W.; Dung, J-S., J. Am. Chem. Soc., 1984, 106, 5748-5750.
`
`*Synthesis and Antimicrobial Evaluation of Bicyclomycin Analogs. Williams, R.M.; Armstrong,
`R.W.; Dung, J-S., J. Med. Chem., 1985, 28, 733-740.
`*Unusual Bridgehead Hydroxylations via Selenoxides: Evidence for Bridgehead Carbocations.
`Williams, R.M.; Dung, J-S., Tetrahedron Lett., 1985, 26, 37-38.
`*A Divergent Generalized Synthesis of Unsymmetrically Substituted 2,5-Piperazinediones.
`Williams, R.M.; Armstrong, R.W.; Maruyama, L.K.; Dung, J-S.; Anderson, O.P., J. Am. Chem.
`Soc., 1985, 107, 3246-3253.
`*Stereocontrolled Total Synthesis of (±)- and (+)-Bicyclomycin. Williams, R.M.; Armstrong, R.W.;
`Dung, J-S., J. Am. Chem. Soc., 1985, 107, 3253-3266.
`*C-Glycosidation of Pyridyl Thioglycosides. Stewart, A.O.; Williams, R.M., J. Am. Chem. Soc.,
`1985, 107, 4289-4296.
`*Thiolate Additions to Bicyclomycin and Analogues: A Structurally Novel Latent Michael-
`Acceptor System. Williams, R.M.; Tomizawa, K.; Armstrong, R.W.; Dung, J-S., J. Am. Chem.
`Soc., 1985, 107, 6419-6421.
`
`*Electrophilic Glycinates: New and Versatile Templates for Asymmetric Amino Acid Synthesis.
`Sinclair, P.J.; Zhai, D.; Reibenspies, J.; Williams, R.M., J. Am. Chem. Soc., 1986, 108, 1103-
`1104.
`
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`23.
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`24.
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`25.
`
`1987
`26.
`
`27.
`
`28.
`
`1988
`29.
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`30.
`
`31.
`
`32.
`
`33.
`
`34.
`
`35.
`
`36.
`
`37.
`
`38.
`
`1989
`39.
`
`
`
`*Promising Cyclization Reactions to Construct the Ring Systems of Brevianamides A,B.
`Williams, R.M.; Glinka, T., Tetrahedron Lett., 1986, 27, 3581-3584.
`*Asymmetric Synthesis of (R)- and (S)-[2-2H1]-Glycine. Williams, R.M.; Zhai, D.; Sinclair, P.J., J.
`Org. Chem., 1986, 51, 5021-5022.
`*Synthesis of a Bicyclo[4.1.1] b-Lactam: A Novel, Anti-Bredt b-Lactam. Williams, R.M.; Lee, B.,
`J. Am. Chem. Soc., 1986, 108, 6431-6433.
`
`*A New Synthetic Approach to 1-Hydroxymethyl-8-methoxy-1,2,3,4-tetrahydro-isoquinolin-4-
`one. Williams, R.M.; Zhai, W.; Ehrlich, P.P.; Hendrix, J., J. Org. Chem., 1987, 52, 2615-2617.
`*Mechanism, Biological Relevance and Structural Requirements for Thiolate Additions to
`Bicyclomycin and Analogues: A Unique Latent Michael Acceptor System. Williams, R.M.;
`Tomizawa, K.; Armstrong, R.W.; Dung, J-S., J. Am. Chem. Soc., 1987, 109, 4028-4035.
`*Synthesis of Functionalized Bicyclic Dioxopiperazines via Intramolecular Epoxide Opening.
`Williams, R.M.; Maruyama, L.K., J. Org. Chem., 1987, 52, 4044-4047.
`
`*Alkynylation of Mixed Haloacetals with Organotin Acetylides. Zhai, D.; Zhai, W.; Williams, R.M.,
`J. Am. Chem. Soc., 1988, 110, 2501-2505.
`*Practical Asymmetric Synthesis of a-Amino Acids through Carbon-Carbon Bond Constructions
`on Electrophilic Glycine Templates. Williams, R.M.; Sinclair, P.J.; Zhai, D.; Chen, D., J. Am.
`Chem. Soc., 1988, 110, 1547-1557.
`*Bicyclomycin: Synthetic, Mechanistic and Biological Studies. Williams, R.M.; Durham, C.A.,
`Chemical Reviews, 1988, 88, 511-540.
`*Asymmetric Synthesis of b-Carboxy Aspartic Acid (Asa). Williams, R.M.; Sinclair, P.J.; Zhai,
`W., J. Am. Chem. Soc., 1988, 110, 482-483.
`*Synthesis of Verruculotoxin. Williams, R.M.; Brunner, E.J.; Sabol, M.R., Synthesis, 1988, 963-
`966.
`*Versatile New Approach to the Synthesis of Monosubstituted and Bicyclic Piperazine-2,5-
`diones: Unusual in situ Generation and Enolate Addition to a Cumulene. Williams, R.M.; Kwast,
`A., J. Org. Chem., 1988, 53, 5785-5787.
`
`*Asymmetric Synthesis of a-Amino Acids: Comparison of Enolate vs Cation Functionalization of
`N-BOC-5,6-Diphenyl-2,3,5,6-tetrahydro-4H-1,4-oxazin-2-ones. Williams, R.M.; Im, M-N.,
`Tetrahedron Lett., 1988, 29, 6075-6078.
`*Versatile, stereocontrolled, Asymmetric Synthesis of E-Vinylglycine Derivatives. Williams, R.M.;
`Zhai, W., Tetrahedron, 1988, 44, 5425-5430.
`*Facial Selectivity of the Intramolecular SN2’ Cyclization: Stereocontrolled Total Synthesis of
`Brevianamide B. Williams, R.M.; Glinka, T.; Kwast, E., J. Am. Chem. Soc., 1988, 110, 5927-
`5929.
`*Synthesis and X-Ray Crystal Structure Determination of 1,3-Bridged b-Lactams: Novel, Anti-
`Bredt b-Lactams. Williams, R.M.; Lee, B-H.; Miller, M.M.; Anderson, O.P., in Recent Advances
`in the Chemistry of b-Lactam Antibiotics, Royal Society of Chemistry, London 1988 pp. 106-118.
`
`*Synthesis and X-Ray Crystal Structure Determination of 1,3-Bridged b-Lactams: Novel, Anti-
`Bredt b-Lactams. Williams, R.M.; Lee, B.H.; Miller, S.; Anderson, O.P., J. Am. Chem. Soc.,
`1989, 111, 1073-1081.
`
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`40.
`
`41.
`
`42.
`
`43.
`
`44.
`
`1990
`45.
`
`46.
`
`47.
`
`48.
`
`49.
`
`50.
`
`51.
`
`1991
`
`52.
`
`53.
`
`54.
`
`55.
`
`56.
`
`57.
`
`
`
`*Carbanion-Mediated Oxidative Deprotection of Non-Enolizable Benzylated Amides. Williams,
`R.M.; Kwast, E., Tetrahedron Lett., 1989, 30, 451-454.
`*Remarkable, Enantio-Divergent Biogenesis of Brevianamide A and B. Williams, R.M.; Kwast,
`E.; Coffman, H.; Glinka, T., J. Am. Chem. Soc., 1989, 111, 3064-3065.
`*Synthetic studies on FR900482: Promising Method to Construct the Bicyclic Hydroxylamine
`Hemi-Ketal Ring System. Yasuda, N.; Williams, R.M., Tetrahedron Lett., 1989, 30, 3397-3400.
`*Synthetic Studies on Paraherquamide: Regioselectivity of Indole Oxidation. Williams, R.M.;
`Glinka, T.; Kwast, E., Tetrahedron Lett., 1989, 30, 5575-5578.
`*Synthesis of Optically Active a-Amino Acids, Williams, R.M., Pergamon Press, 1989, Oxford,
`(Organic Chemistry Series, Baldwin, J.E., Series Editor). 410 pp.
`
`*Synthesis of Ethynylglycine (FR900130). Williams, R.M.;Aldous, D.J.; Aldous, S.C., J. Chem.
`Soc. Perkin Trans I Comm., 1990, 171-172.
`*Asymmetric Synthesis of Arylglycines. Williams, R.M.; Hendrix, J.A., J. Org. Chem., 1990, 55,
`3723-3728.
`
`*Asymmetric, Stereocontrolled Total Synthesis of (-)-Brevianamide B. Williams, R.M.; Glinka, T.;
`Kwast, E.; Coffman, H.; Stille, J.K., J. Am. Chem. Soc., 1990, 112, 808-821.
`*General Synthesis of b,g-Alkynylglycine Derivatives. Williams, R.M.; Aldous, D.J.; Aldous, S.C.,
`J. Org. Chem., 1990, 55, 4657-4663.
`*Synthetic Studies on Aspirochlorine (A30641). Williams, R.M.; Miknis, G.F., Tetrahedron Lett.,
`1990, 31, 4297-4300.
`*Synthetic Studies on Paraherquamide: Synthesis of the 2H-1,5-Benzodioxepin Ring System.
`Williams, R.M.; Cushing, T.D., Tetrahedron Lett., 1990, 31, 6325-6328.
`*Identification of a Novel Structural Class of Positive Modulators of the N-Methyl-D-Aspartate
`Receptor, Whose Actions are Mediated Through the Glycine Recognition Site. Monahan, J.B.;
`Hood, W.F.; Compton, R.P.; Cordi, A.A.; Williams, R.M., Eur. J. Pharmacol., 1990, 189, 373-
`379.
`
`∫Highly Stereoselective Synthesis of Conjugated E,E- and E,Z-Dienes, E-Enynes and E-1,2,3-
`Butatrienes via Alkenylborane Derivatives. Negishi, E.; Yoshida, T.; Abramovitch, A.; Lew, G.;
`Williams, R.M., Tetrahedron, 1991, 47, 343-356.
`*Synthesis, Conformation, Crystal Structures and DNA Cleavage Abilities of Tetracyclic Analogs
`of Quinocarcin. Williams, R.M.; Glinka, T.; Gallegos, R.; Ehrlich, P.; Flanagan, M.E.; Coffman,
`H.; Park, G., Tetrahedron (Symposium-in-Print), 1991, 47, 2629-2642.
`*Synthesis of Tri-Substituted Furans: Mild Ti(IV)-Mediated Couplings to Acetals. Construction of
`the Epoxy Hemi-Amido Ketal of Fusarin C. Williams, R.M.; Esslinger, C.S., Tetrahedron Lett.,
`1991, 32, 3635-3638.
`*Novel Ring Contractions via 2,3-Wittig Rearrangements: Synthesis of (2-Desoxy)-2-Methylene
`Bicyclomycin. Williams, R.M.; Sabol, M.R.; Kim, H.; Kwast, A., J. Am. Chem. Soc., 1991, 113,
`6621-6633.
`*Asymmetric Synthesis of 2,6-Diamino-6-hydroxymethylpimelic Acid: Assignment of
`Stereochemistry. Williams, R.M.; Im, M-N.; Cao, J., J. Am. Chem. Soc., 1991, 113, 6976-6981.
`*Asymmetric Synthesis of 1-Aminocyclopropane Carboxylic Acid Derivatives. Williams, R.M.;
`Fegley, G.J., J. Am. Chem. Soc., 1991, 113, 8796-8806.
`
`10
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`58.
`
`59.
`
`1992
`60.
`
`61.
`62.
`
`63.
`
`64.
`
`65.
`
`66.
`
`67.
`
`68.
`
`69.
`
`70.
`
`1993
`71.
`
`72.
`
`73.
`
`74.
`
`75.
`
`76.
`
`
`
`*Asymmetric Synthesis of Mono-Substituted and a,a-Disubstituted a-Amino Acids via
`Diastereoselective Glycine Enolate Alkylations. Williams, R.M.; Im, M-N., J. Am. Chem. Soc.,
`1991, 113, 9276-9286.
`*Cannizzaro-Based O2-Dependent Cleavage of DNA by Quinocarcin. Williams, R.M.; Glinka, T.;
`Flanagan, M.E.; Gallegos, R.; Coffman, H.; Pei, D., Advances in New Drug Development, The
`Pharmaceutical Society of Korea, Seoul 1991, 38-50.
`
`*Cannizzaro-Based O2-Dependent Cleavage of DNA by Quinocarcin. Williams, R.M.; Glinka, T.;
`Flanagan, M.E.; Gallegos, R.; Coffman, H.; Pei, D., J. Am. Chem. Soc., 1992, 114, 733-740.
`*Asymmetric Synthesis of a-Amino Acids. Williams, R.M., Aldrichimica Acta, 1992, 25, 11-25.
`*Preparation of 4-Methoxy-4’-nitrobiphenyl. Stille, J.K.; Echavarren, A.M.; Williams, R.M.;
`Hendrix, J.A., Org. Synth., 1992, 71, 97-106.
`*Asymmetric Synthesis of Arylglycines. Williams, R.M.; Hendrix, J.A., Chem. Rev., 1992, 92,
`889-917.
`*DNA Cross-Linking Studies on FR-900482: Observations on the Mode of Activation. Williams,
`R.M.; Rajski, S.R., Tetrahedron Lett., 1992, 33, 2929-2932.
`*Asymmetric Synthesis of 2,6-Diaminopimelic Acids. Williams, R.M.; Yuan, C., J. Org. Chem.,
`1992, 57, 6519-6527.
`*Asymmetric Synthesis of S-(-)-Cucurbitine. Williams, R.M.; Fegley, G.J., Tetrahedron Lett.,
`1992, 33, 6755-6758.
`*Asymmetric [1,3]-Dipolar Cycloaddition Reactions: Synthesis of Highly Subst