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`2,3,3-Er,me-3491S(1) 15.9 g (0.1 mol)S
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`
`d), 6.86C]H,
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`+ 161
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`: 1.09(3H, s), 1,2103H, d), 1.32(3H. s), 3.63(1H, a), 4.07CH, br. s), 7.08(1H,
`
`d), 7.36C1I, d), 7.62(1II, dd)
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`: 206
`
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`
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`[0084]
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`£0089]
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`[0094]
`
`[0096]
`
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`(58.1 )& SRAr}.
`
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`
`: 846
`
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`[0098]
`
`[0099]
`
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`
`> 322
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`
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`
`[0105]
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`
`: 722
`
`[0107]
`
`[A] 3] 1,3-8]2-[6-(}°] 22 449}4] &)-2,3-] spo] 22-2,3,3-Ez] W] S-1-(1-3] dq] 2)1 NS-5-F)-
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`(10) gal
`
`-14-
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`
`Ethyl acetate
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`
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`
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`
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`
`+ 390
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`BLS2. 13-4] 2:-[6-C}o] 234 o} u] &)-2, 3-U spol E B-2 3. 3-E a] ol S-1-C-F 92-1 91S
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`[0109]
`
`fOL10]
`
`fO111]
`
`f0112]
`
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`
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`
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`
`[0116]
`
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`
`(01194
`
`10120]
`
`[0121]
`
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`
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`
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`: 858
`
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`(5.0 mol) So}e]°]E 20
`
`-15-
`
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`(12) 1.80 g (92.3 2 Ad.
`
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`
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`
`[0122] MS(a/e)>390
`
`BRG2. 1.3-4) 4-[6-(Apo] Fe MEO} a] SOFT]
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`
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`
`[0126]
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`{0127]
`
`[0129]
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`[0132]
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`
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`
`(13) 1.21 g (61.4 ®)& YBrH.
`
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`
`: 858
`
`[AA]o] 5] 1,3-4]2-[6-(2,2,2-B2S9Sopa] 2 ofa] & )-2,3-T]s}o] =S-2,3,3-B ez] i] B-1-(1-H] de] 2 )-1
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`
`7
`H3G-CH-Pn
`(5)
`
`(CFiC)0
`Ethyl acetate
`
`9
`F3CCHN
`
`N
`H3C~CH-Ph
`
`(14)
`
`2 iow
`2
`eck De FA EWSSOLS1.05 g (6.0ano) %aaa PAG WSS] SLA ens 943]
`
`S}o] S S-2 3,3-Ee) yy) S-1-(1-e) So) S)-14 2165) 1.4 g (65.0 mol) Weo}alele
`a
`Te
`
`Ww
`
`A,
`
`IA Zt Set abs. UU oS, SHS 50 MS BSS] RAS] May Bar 20H Sot my F Hs
`
`& Ess Sack fe] We 48, IFS HSS SY Sisto] Voll wa wae Ase] 4
`
`
`S se) 29,9Bas 2o2-¥[2,3-c spol = e-2 3,3-Ee] qe-1-(1-] 4] S)-17-21 5-6-4 J-o} 4] Eo}
`J}E(14) 1.71 g
`(91.0 He Agr}
`
`S(a/e)
`
`{0133]
`
`{G133]
`
`
`BES2
`13-0) 2:-[6-(2,2,2-Eg S32 Go} a] go} ey]
`S-U spo] E-2 3 3-Ee] ey e-1-(-#] ao
`
`Oo
`il
`—-HyCCHN
`
`N
`;
`
`

`

`
`
`
`B-1 1S5-9 |- to} C15) Sd
`
`olf ht Jil ol 10- 1842495
`
`.
`Oo.
`HO.
`Y
`Triethylorthoformate
`
`
`g ||——+
`
`F3CCHN
`N
`‘
`EtOH
`
`
`
`[0136]
`
`[0137]
`
`[0138]
`
`fO140]
`
`70141]
`
`(15)
`
`
`2,2,2-EBq]S72=2-M[2,3-eo LS-2,3,3-Ez] gq] e-L 1-H So 2 )-LF aS-6- 2-9} A Bo}fo] & (14)
`1.50 g (4.0 mol FE JBL 40 mle] BAaly|a AoA, 304 Ee
`SH OS, 2toPelA 0.23 g
`=
`(2.0 mnol)#} S2=REXSAEGQIS 2.3 ol
`(13.18 mnol)& +a 7st BVH S AAS] SS 4471 |S
`Qt SHS SAT}. HOES Jel V4 % 444 a4] VAISS Feo WASH of Ww NTe -
`
`Aza] Aa ZZ] 1,3-]A-[6-(2,2,2-H SHO Hop eo}y]-)-2,3-K] so] 2S-2,3,3-H a]-1-
`
`(1-3 2-1 eS-5- & ]- 20/4 (15) 0.85 g (51.38 He AMF.
`
`MALDI-TOF MSGm/e)
`
`: 830
`
`[AA] 4] 6] 1,3-8]2-[6-( 29 O}7] &)-2,3-4 spo] ES-1-(1-F] dB)1 NS-5-A 1-2FS (20) 2] AA
`
`Bee]. 6-UES-2,3-t spo]S-1-C-s]
`4 2)-1F EAD 4
`
`
`
`_PHCU(CHSBr\Br wee
`
`DIPEA.DMEDME
`O2N
`NH
`H3C-da.Ph
`(17)
`
`[0142]
`
`(0143)
`
`[0144]
`
`[0145]
`
`[0147]
`
`[0143]
`
`70149]
`
`(16)
`
`AAA) SelAl 6-YES-2,3-sp>o) 22-147 21S(16) 10.0 g (0.061 mol IS AASYSHIE 100 mle] #
`APAZ|] aL ALSO A, 10 BE pS OS, (1-HEOE)12.6 g (0.068 mol) FlAZ SY] So}F
`
`(DIPEA) 12.4 ml
`(0.073 mol)& AE 7A SB MESS ars] SLs} 100 “CoAl 5AZE St TBks}oF
`Des tasae. WSS ALLE BASE
`OF SRS 100 mls} ayelotaleol 200 ml 7hsboy-Fat 30%
`
`ee wks} f7Se det - HOE S24 V1 OF, ISt Ss Feesess AzsaD
`
`ay Sree] SS a4] AVES WES 50 mle] TA) 7] oesueUne F spss AASpo
`‘E NMRC& ppm; CDCls3)
`:
`1.58¢8H, d), 2.97-3.07(2H, m), 8.40-3.45(]H, m), 3.56(]H, q), 4.82(1H, q),
`
`
`
`7.07C1H, dt), 7.11C1H, d), 7.26-7.30(01H, m), 7.34-7.38(4H, m), 7.48C1H, dd)
`
`MS(m/e)
`
`: 268
`
` I
`
`HaC-CH-Ph
`{17)
`
`-CH-
`H3C-CH-Ph
`(18}
`
`10.2 g (0.088 mol) S FARZI]Sat ae.
`6-YES-2,3-s}o]) 2 S-1-(1- sd S)-14 91017)
`aA &,
`10% Pa/C Bry 0.5 gt} SA VAS yeaCS AoA 154/71
`Se
`Ffpspo] Sus Alsi BS We} Sirs] AM Arye] 6-ofe]-2, 3-1] so]
`
`-17-
`
`

`

`(18) 7.80 g (86.3 %)S Sry.
`
`[0150]
`
`y NMRCOS& ppm; CDCl3)
`
`: 1.53(3H, d), 2.85(2H,
`
`t), 3.300C1H. q), 3.38(1H, q), 3.46(2H, br. s), 4.68C1H,
`
`qa), 5.78(1H, d), 5.9701H, dd), 6.84C0H, d), 7.25-7.42(5H, m)
`
`MSGm/e)
`
`: 238
`
`hes. AM[2 3-1) fo]1-1-9) ol 2) Wr gh-6- 2 | 20}ubo] (19) ed
`
`fO1S1]
`
`[0153]
`
`SSSOl 10-1842495
`
`ql
`aool
`
`(0154]
`
`[0155]
`
`HoN
`
`N
`H3C-CH-Ph
`
`(18}
`
`CH2CI;
`
`PhOCIIN
`
`N
`HiC-CHEPh
`
`{19)
`
`
`BES -5 CH F278 GS, Exqeorsl 0.7 ml
`(5.0 mmol) S 7A WSIS lO Bot abe *
`
`
`6-oFU] -2, 8-C] spo] EF-1-(1-F] S4] S)-1F2S(18) 1.2 g (5.0nmol S2298 15 nlSaAyzjz
`Asq“49 0.7 g (5.0 mol)S AAS FeBu Beso] 9-347 SES SISA 1A] Sek agrayr}
`
`2a 08, 28 50 mS Usk AAS Fata 30H Set WU = FASS Beaw SHSE FAW
`
`Nose tps, sre wis ae BHspoy Aozl wal AYBLS Azo) ESS Yo#u AAG Ae
`
`Bae] M[2,3-T] so] ES-1-(1-s do S)-1 91S-6- 2] offo] E19) 1.19 g (69.6 HS SBr}
`
`{0156]
`
`Tl NMRCS ppm; CDCl3)
`
`: 1.56(3I, d), 2.91021],
`
`t), 3.3001, qa), 3.45011], a), 4.83011],
`
`aq), 6.76C1Il, d),
`
`6.93(1H, s), 7.00(01H, d), 7.25- 7.55(8H, m), 7.73(1H, s), 7.83-7.85(2H, m)
`
`MS(a/e)
`
`: 342
`
`
`BhS4. 13-8] 2-[6-(al29lo}u]tc)-2,3-] sto] 22 1-(1-w] ol e))~ ee)5-9) |-20h) (20) aha
`
`[0157]
`
`[0159]
`
`{0160}
`
`(0161)
`
`[0162]
`
`[0164]
`
`oe rE Triethylorthoformatese
`
`HO,
`
`HO
`
`.
`
`O
`
`°
`
`EtOH
`
`PhOCHN
`
`N
`H3C~CH-Ph
`
`(19)
`
`o
`
`68
`(20)
`
`H3CHC
`
`
`
`A-[2,3-U]3}o]) £S-1-(-3)4S )-1491S-6-F |WZe}spo] E19) 1.10 g (3.2 mnol) Hee ERS 30 ml
`BAAS ALA] 30 Bet TRS che, SPORa 0.18 g (1.6 mmol)4} QB2E¥SAEzye 1.8 ml
`(10.8 mmol)& *-= 7palseat WSSS AALS) SS}O4 WaSot BAUR site Were aetou Wy
`2 = HA Da AGES Fypspa WSS oe]a Wols - Aspe] lsb aaae 1,3-4] 2-[6-(A
`
`2] oF] & )-2 ,3-C] so] ES-1-C1-] So] 1) - 191S-5- 2 J- 4540421 $20) 0.65 g
`
`(53.3 HS AArt.
`
`MALDI-TOF MSGm/e)
`
`: 762
`
`7]
`
`1,3-8]2-[6-(4] so}2 Fe]: )-2, 3-C] 89] =S-1-(1-3] 3B)-1 1S-5-S )-2FOFSF (22) 2]
`
`[AA eo]
`Ale
`
`-18-
`
`

`

`10165]
`
`BeS1 (2, 3-c] spo] = -1- (1-9 dol B)- 191 8-6-9 J- w]e} al elobpo] E21) Bg
`
`
`
`
`SSS 10-1842495
`
`ID “GLeL ioei
`
`i
`
`CTLCl,
`7+
`
`HN
`
`"
`I
`H3G~CH-Ph
`(18)
`
`
`
`PhH2COCHN
`
`N
`HaC-CH-Ph
`QU
`
`[0166]
`
`[0167]
`
`[0169]
`
`f0171]
`
`[0172]
`
`[0173]
`
`[0174]
`
`[0176]
`
`[0177]
`
`[0178]
`
`fO179]
`
`6-OF8] 4-2, 3-F] Spo] GS-1-C1- 9] 44) B)-1F VSC8) 1.2 g (5.0 mol) FSB2=Hr4 15 ml Sea 71a
`
`
`
`Baa) So}2 0.77 g (5.0 mmol) S AAS FAFSA WSS] SES] SES SSAA LASet Best
`
`(5.0 mol)S 7AFa UWSSAS lok Sel aye F
`Wmees -5 CH wae oe, EzSeoesl 0.7 ml
`ar. 2a es, ane 50 mS VSSo] AAS] Fafa 20% Sok DY * GrlSe Basa SHER OF
`
`Yow We
`US, Bet HSS 2H Sra Sq a4] YVSS ABS YBSE AUG AHI
`
`qa weale] [2,3-dsbe]=-1-(-s]¥o] S)-14 91 S-6-2 J -sl opSobbo] E21)
`«1.11 g 62.5 HS
`2 Qc}
`
`[6168]
`
`H NMRC& ppm; CDCl3)
`
`: 1.50(3H, d), 2.85(2H,
`
`t), 3.23CH, q), 3.88C1H, q), 3.69(2H, s), 4.76C1H, q),
`
`6.450H, d), 6.74C1H, d), 6.89C1H, d), 6.99(1H, s), 7.23-7.40(C10H, m)
`
`MS(m/e)
`
`> 356
`
`
`
`
`
`WeS2, 13-0] A-[6-(ai)t ob a] elo} )-2, 3-0] sho) F-1-(1- 3) ol)“1-5-9) | Ato} (22) Bh
`
`PhH,COCHN
`
`|
`N
`HsC-CHPh
`(21)
`
`HsO
`
`4
`
`HO
`
`..
`Triethylorthoformate——
`E:OH
`
`o
`
`°
`
`9
`
`t
`
`NHCCHPh CH,
`
`(22)
`
`
`spol =B-1-(1-F] oy a)1 S-6-9 |- wy sop] oppo] E21) 1.0 g (2.8 mmol)S
`
`oo wea tio (i,roft |O.Hloe
`ml el ee ASA] 30% Set aS THR, AAPOPeAP 0.16 g (1.4 mmol)#} SSREREAEE
`mol) Ape) ent Wees AAS] SLsoH AA|zb Sek Sires st
`41 na) ASSS Asstt RSH de] WH Rose + A
`dob obF] =)-2,3-F] 3}>| 8-1(-a) dalerelSs“A )-AsohS3
`
`co
`
`4
`
`(ALDI-TOF MS(n/e)
`
`: 790
`
`[AA] 4] 8] 13-8] 2-[6-(o}4] 2 ofe] &)-2,3-T] apo] =2-1-(1-¥] Yo] 2) -1 91S-5-S ]-AFo} a FH (24) 9] AH
`
`Gkel. A [2,3-T]epo] ©1-1-3 9] 2) 19) 6-9 J-o} i] ofbo) (23) etd
`
`H2N
`
`9g
`
`
`
`CH,CCIrrN CH2Cl,
`
`H3COCHN
`
`HsC-CHPh
`
`(18)
`
`LD
`
`‘
`HaC-Ch-Ph
`
`(23)
`
`6-O-2] 4-2, 3-F] So] E S-1-(1-F] do) B)-1F 1S 8) 1.2 g (5.0 mol) S FSH2=2595 15 mia Sa A 71a
`
`BeeS -5 CH FAH US, Eeqeops 0.7 ml
`(5.0 mol) 7a we 8
`
`Satoh 0.39 ¢g
`(5.0 mol)S AAS Fafa USE] SLa74) YES
`
`-19-
`
`

`

`SSS 10-1842495
`
`
`
`[0180]
`
`y NMRC6& ppm; CDCls)
`
`: 1.53(3H, d), 2.11(3H, s), 2.88(2H,
`
`t), 3.29C1H, q), 3.42(1H, a), 4.75C1H. q),
`
`fO181]
`
`f0183]
`
`f0184]
`
`TOLRS)]
`
`fOLR6]
`
`[0188]
`
`[0189]
`
`f0190]
`
`[0191]
`
`6.610H, d), 6.7001H, s), 6.94C1H, d), 7.0501H, s), 7.24-7.39(6H, m)
`
`MSGmn/e)
`
`: 280
`
`
`
`
`1. B-H]A-[6-(o}-¥)] So} M] xe )-2,g-1] spo] = 1s) oy) ye-5-V Ato} B24) Fh
`uLS2.
`
`Al
`
`H3COCHN
`
`N
`H3C-CH-Ph
`
`oe 1 Ft Triethylorthoformateee
`
`H20.
`
`Ho
`
`.
`
`oO
`
`6
`
`EtOH
`
`(23)
`
`
`
`M-[2,3-ao) E#-1-(1-s] do] 8)
`-6-2 berale e+e}°] = (23) 1.0 g (3.6 mmole EE WES 30 ml
`ol] BAbaly]at AoA 30H Eek aS THE, AAPoPelAA 0.21 g (1.8 mmol)#} PSEVSEAER
`(12.6 mons ase] 7a BSSS AAS] SLs] 44/71 Sel SHUG stir}. USES
`a
`Bobups)-2,3-4 spo] SS-1-(1-a] Ao] BUs-5-F |-AFPora(24) 0.61 g (53.0 %)S ase
`
`4-2 S42 Da AQGS Ges WSS 4B YW Ve — AzAG BS49] 1,3-
`
`MALDI-TOF MS(m/e)
`
`: 638
`
`[AAle] 9] 1,3-8]2-[6-bo] 234 o}n]&)-2, 3-c] spo] =B-1-(1-3] Yo] B)-14- 91S-5-S ]-2Hope)(26) S]
`ALA
`
`
`
`Gkel. M[2,3-t] spo] =S11 sl)ol) 2) WF 3)6-2 | -Ab 0] a Sh} eo}ero] (25) ghd
`
`HN
`
`N
`H3C-CH-Ph
`(18)
`
`1CCl
`
`CH>Cl,
`
`-
`
`4
`©—CHN
`
`N
`HaG-CH-Ph
`(25)
`
`6-9} F] 2-2, 3-3} o] = S-1-(1-A ee S)-1F 728) 1.2 ¢ 6.0 ool) S FARE 15 mld SAA 7a
`
`(5.0 mmol) *Paystar HPS BAS 10H Sok ae =F
`WES -5 CH FAM OS, Eel] eorel 0.7 ml
`AsppoSeaat7yeny 0.73 g (5.0 mol)& AAS FSU MPSS] S254) FESR FSA LIZ
`Sok DHA. I US, SH50 mS BS So] AAS 7st 20H Sek wet S FolSS Helsa
`
`SATS 44H AVS OS, Bat 7"188 OU SRYA a4 AASS AGS] WASH As
`
`Axes] SA LAA] [2,3-cClspo] =
`1.28 g (73.6 2 UH
`
`
`S-1-(1-H 4d S)-1FUS-6-F Apo SSAASo}of 9] = (25)
`
`[0192]
`
`‘a NMR(& ppm; CDCl3)
`
`: 1.22-1.34(3H, m), 1.49-1.95(10H, m), 2.17(1H,
`
`t), 3.23(1H, q),
`
`tt), 2.87(2H,
`,
`
`3.39C]H, q), 4.8101H, q), 6.60(1H, d), 6.87(1H, s), 6.94C1H, d), 7.06(1H,
`
`$s),
`
`7.24-7.39(5H, m)
`
`f0193]
`
`[0195]
`
`MS(a/e)
`
`> 348
`
`
`
`13-0] A-[6-VA}o] $88] Je) ] we), 3-1] 3) 2-]-(sf)of) 19) B52) | -2 Fh0)}
`whB2.
`
`—-?0-
`
`

`

`(26) #4
`
`SSS 10-1842495
`
`.
`°
`H,0
`Il Uaoc
`
`
`C-CHN
`"
`EtOH
`H3C-CH-Ph
`(25)
`
`Oo TD 4
`
`Tnethylorthoformate
`
`HO
`
`°
`
`
`
`(26)
`
`
`A-[2,38-0 sho] 22-1-(1- 4] 4) 4-14 21 S-6-4 -A}9) S 2A SofPP Oo] E (25) 1.25 g (3.6 mole Be
`yes 30 mle] B44] 7) at AeA] 308 Sok BLES CHS, Aste-e At 0.21 g (1.8 mmol) ¥} SSEMSAE
`ve
`m
`Bch. Wess
`
`12.6 ms “ya rel TOES AAS] Sesto] AASE SapekS St
`
`1
`
`MALDI-TOF MSGn/e)
`
`: 774
`
`10] 1,3-8)2-[6-Afo]2 eto}4] Bo}o] &)-2, 3-0] spo] HS-1-(1-3] do) -1 91S-5-9 J-2ope
`[AAle]
`H(28)2] Ae
`
`
`
` 4
`
`° LOUl
`Decrtic:
`Ee o lgCCIIN
`N
`CH2Ch
`HeC-CH-Ph
`
`(27)
`
`H2N
`
`ow
`H3C-CH-Ph
`1g)
`
`6-O-F] 22-2, 3-F spo] = S-1-(1-F] So 2 )-1F 2e8) 1.2 ¢ 6.0 ool) & FSABE7% 15 mlSAA 7) aL
`
`
`Asso] Sea sop e 0.73 g (5.0 mol)& AA8) 7a WS Se] S252] SER FESPA 1A |
`
`
`(5.0 mens FyAFW USSAS le Set ayer &
`WES -5 CH H2)3 FS, Helo eopyl 0.7 mi
`gh aes. LeSAS 50 mis RSS AAol oie a 30% SS) GR FE Ss esta |
`
`wee FW Ade the, Ao les GH Sree Cd wa VES 2Ee] WSS QUAL
`
`azyq At wee} M[2,3-lspo)Se-1-(1- AeS)-14 1 S-6-Z]-Afo] SHBofA] Bopupo] = (27)
`1.30 g (74.7 H)S UMr}.
`
`[0196]
`
`[0197]
`
`(0198)
`
`{6200]
`
`10201]
`
`[0202]
`
`[0203]
`
`[0204]
`
`4 NMRC& ppm; CDC1;)
`
`: 1.17-1.21(2H, m), 1.52(8H, d), 1.56-1.66(4H, m), 1.86-1.90(2H, m), 2.27-
`
`t), 3.25C1H, q), 3.40€1H,
`2.36(3H, m), 2.87(2H,
`d), 6.99(1H, s), 7.23-7.39(5H, m)
`
`MS(a/e)
`
`: 348
`
`q), 4.79(1H,
`
`gq), 6.60(1H, d), 6.79C1H, s), 6.94(]H,
`
`
`
`hed. 1,3-4) 4-[6-C}o] 3 3 olFo} 4] S oF] & )-2 3-T] spo] EB- 1-1-3 0) 2-1 9-5-9 J 2OS (28)
`ay
`g
`
`1a
`
`oo
`¢
`
`

`

`[0208]
`
`[0269]
`
`10210]
`
`[0212]
`
`10213]
`
`[0214]
`
`{0215}
`
`(0216)
`
`[0217]
`
`[0219]
`
`SSS 10-1842495
`
`i
`°
`HyCCHN
`
`|
`
`"
`
`HO
`
`OQ
`
`.
`.
`
`Triethylorthoformate
`EtOH
`
`50 ~CH-
`
`JES 30 mle] #4bly|at ALA 305 SSk BBS: THB, AAPoPa*t 0.21 g (1.8 mnol)>} SSEY EAE
`
`HESoTse Sealer)ue S-6-Y]-A}9°) SSlops] Eofofo]E(27) 1.25 g (3.6 molle FS
`Ze 2.1 ml
`(12.6 m abe a}a wale Wee Ae] SSS] 44/7 SS BHUES SHAcH. “
`£4228 a4 =e lela aA) AASS Axe WASH fe] Ale - Asse Ae ASM) 1
`4]2-[6-(A}o] Sal eto}4]2ofa])-2,3-1]3}=s-1-(1-s3e] 2)-144) aL220}(28)
`0.81
`
`gQ
`
`(58.4 H)& ABry.
`
`MALDI-TOF MSCm/e)
`
`= 774
`
`[al] 11] 1,3-4]2-[6-(2,2,2-E S92Sof] Bo}4] &)-2,3-c] so] =B-1-(1-3] 2] B)-1F US-5-S J -4
`HoFSH(30)2] ae
`
`
`
`
`
`Oo
`
`HoN
`
`ee
`CHCl
`F,CCHN
`
`N
`H3C~CH-Ph
`
`(18)
`
`N
`H3C~CH-Ph
`
`(29)
`
`6-OF2] 4-2, 3-T] df 0] S S-1-(1-4] So] B)-1F DSC8) 1.2 g (5.0 mol)S FSB4 15 mld Sa71a
`
`(5.0 mol)S 7Fat WSLRAS 10% Sel Wes
`Bees -5 CH Hz)oS, Eesope 0.7 ml
`Ur EYSFoBztt 1.05 g (5.0 mol)S AAS 7S)F Wee] $234 SES FASHHA VIZ |Set
`weg, 2A OS, Sip 50 mS WES] AAS) Waa 20 Sek wR FS HSS Les SF
`ee Fe] Ne 8, etd TISs GU Sisto CoA Wa] MASS 2GS] MBSE Bot A
`
`
`BSA - eae] 2,2,2-EySeee-i[2,32-cspelee-1(1-ael a)1 S-6-4]-ofa Eohepo] =
`
`(29) 1.24
`
`g (74.3 ®)& WBr}
`
`II NRCS ppm; CDCl3)
`
`: 1.55¢80, d), 2.93(21,
`
`t), 3.35010, a), 3.48011, q), 4.75(1I], q), 6.66-6.68(2I],
`
`m), 6.99C1H, d), 7.25-7.39(5H, m), 7.70(1H, s)
`
`MS(m/e)
`
`+ 334
`
`
`Weg2. 1 3-s]2-[6-@ 2,2 Bd SpeSopa] gop}: )-2, 3-t] spo] B- 1-1-dol] S 1 els-5- 2| 2 tof
`$(80) 34)
`
`— PD? -
`
`

`

`H,0
`
`o
`
`SSS 10-1842495
`
`HgG-CH-Ph=HO °
`
`.
`.
`Triethylorthoformate
`+
`9
`N
`EtOH
`F3CCHN
`
`(29)
`
` Vl
`
`NHCCF3
`
`Ph|
`CHCH3
`
`=A"
`
`H3CHG
`Ph
`
`I
`
`(30)
`
`[0220]
`
`[0221]
`
`£0222]
`
`{0224]
`
`
`2,2,2-EVS9%92-¥[2,3-c] do] S-1-(1-a) dol 2-1 1 S-6-F |-ofEbbo] = (29) 1.20 g (3.6 mmol)
`
`& FF ES 30 - EAMASL ALMA BO Sk ALVES HHS, AMPA 0.21 g (1.8 amoDt QE
`
`Hees dees 14 F d