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普拉格雷的合成
引用本文:彭锡江,刘烽,何锡敏,潘仙华.普拉格雷的合成[J].精细化工,2011,28(2):156-161.
作者姓名:彭锡江  刘烽  何锡敏  潘仙华
作者单位:上海应用技术学院,香料香精技术与工程学院,上海,200235
摘    要:以4,5,6,7-四氢噻吩并3,2-c]吡啶为起始原料,经苄基保护、溴化、醚化和脱保护4步反应得到2-甲氧基-4,5,6,7-四氢噻吩并3,2-c]吡啶(Ⅺ);以邻氟苄溴为原料,经过格氏缩合、溴代两步反应,得到α-环丙羰基-2-氟苄溴(ⅩⅢ);将该两个化合物再经缩合反应、水解反应和乙酰化反应,以34.6%总收率得到目标化合物;其中部分中间体和目标化合物的结构经1HNMR和MS等进行了表征。

关 键 词:抗血栓  α-环丙羰基-2-氟苄溴  4  5  6  7-四氢噻吩并[3  2-c]吡啶  普拉格雷  医药与日化原料

Synthesis of Prasugrel
PENG Xi-jiang,LIU Feng,HE Xi-min,PAN Xian-hua.Synthesis of Prasugrel[J].Fine Chemicals,2011,28(2):156-161.
Authors:PENG Xi-jiang  LIU Feng  HE Xi-min  PAN Xian-hua
Affiliation:PENG Xi-jiang,LIU Feng,HE Xi-min,PAN Xian-hua(School of Perfume and Aroma Technology,Shanghai Institute of Technology,Shanghai 200235,China)
Abstract:The condensation precursor(Ⅺ) was synthesized via four steps from 4,5,6,7-tetrahydrothienopyridine hydrochloride.Another precursor(Ⅹ Ⅲ) of the condensation reaction was synthesized via two steps from 1-(bromomethyl)-2-fluorobenzene.The target product was prepared via condensation,hydrolysis and acetylation reactions from the two precursors.The yield is 34.6% in the overall seven steps.Some intermediates and target product were identified by 1HNMR and MS.
Keywords:anti-thrombosis  2-bromo-1-cyclopropyl-2-(2-fluorophenyl)ethanone  4  5  6  7-tetra-hydrothieno pyridine  prasugrel  drug and cosmetic materials  
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