西司他丁钠的合成

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1、摘要THESYNTHESISOFCILASTATINSODn见证ABSTRACT111isdiss嘶撕onfocuscdon廿1esynmcSisof④一2，2·dim甜1ylcyClopropanecarboxamideutilizingc：hi】锄reagentS讥aseveralSteps．And也es)，IlmeSisofdlaSta6nsodium晚Ⅱted缸》m(固一2，2·dime也ylcyClopropanecarbox锄ide、7·c1110r0-2一oxoheptanoateemylesterand三一cysteine，

2、andwIliChgavetlleprodllCtin也eoptiⅡ1a1conditions．FiIstly；2，2-dimethylcyclopr．0panecarboxylicacidwasresolVedbyC】血诅1，1’．binaphth01d耐VatiVeSSuCh笛僻)一1，1’-bin印h吐10l，僻)-1，1’-biIlaphm01monomedlylemeror俾)一1，1’—bin印h血olmonoenlyletll％缸d(回-2，2-池甜1ylcyclopropanecarbox锄idew硒obtained丽也18

3、．1％一33．7％yields访aⅡ1r∞st印s：fonnedest盯diaLster∞merS，recrystallization0r∞lu玎蛆chromato伊aphys印ar撕on，and锄monolysis．Then'也es)，ntllesisof(两-2，2一dimemylcyCloprop趾ec曲ox锄idestarted6．om2，2-池甜1ylcyCloprop趾eca而oxylicacidandquil血hne讥athI。eestcps：formedesterdiaSt跚mers，recryStalliza五ons印ar

4、ation，锄d锄onolySis．Andt11etotalyieldof也et11reestepswaS20．5％．Atlast'wer印ortedtwom劬odSformeresol谢onof2，2一dinl如ylcyclopropanec曲oxylic撕d'wh痂山e三一phenyl酉ydnemetllylesterwastllech砌auxiliary'诵t115．8％)，ield访asomest印s：convertedt0aCidc：hloride，recryStalliz撕ons印aration，Ho缸血趾rea玎angemen

5、treactionands印011i丘c撕。玛ect；0r丽tll6．6％)，ieldviaseveralsteps：卸monolysis，rec巧stallizationsepar撕on'saponi丘cationandoxidation．Cila站撕nsodiumw硒synthesized啊atowst印s．FirStly，(回一2，2一dimethylcyclopropanecarboxamidew弱reacted、析血7一chlor0—2一oxoh印tanoateemylesterw11ichgaveethyl7一chloro一2一

6、((1p-2，2-dimemylcyclopropaIlecarbox锄ide)-2·oxoheptanoateethyleSter．Secondly，alkylcilaSta：tillesterwaSproducedby也eHAbsn_actreactionof三-cySteinemethyleSterhydrochloride纽dhetenoicesteriIldiljE旨entconditions．Anda1]哪cil豁tadnesterw弱syn也esizcd、7I，i也74．1％姐eldin也e0I廊a1routeatamater

7、ialralioof1．5：l1lSingK3P04aS出aliVia4eqmVal朗tsat80oCunderTHF勰solvent．Cilasta：tjnsodillmw嬲0bt咖edbysaponi6ca：tionwim49．6％姐eld．111t：hispaper'syntheSisofaIk姐cilaLsta_tineSterw嬲aVoidcdtheuseofs拄ongealkali翘danhydrollsreaCtion∞nditionsinmereactionsyStem，andtherea砸0nC0nmtionsweremn

8、也sinlpleop硎onandmoresujta：bleforiIldllstrialproduction．1'hes仃u酿玳ofproducesw弱confirmcdby1m