广州化工
廣州化工
엄주화공
GUANGZHOU CHEMICAL INDUSTRY AND TECHNOLOGY
2012年
7期
83-84,115
,共3页
Wittig反应%立体选择%Combretastatin%A-4
Wittig反應%立體選擇%Combretastatin%A-4
Wittig반응%입체선택%Combretastatin%A-4
Wittig reaction%stereoselectivity%Combretastatin A-4
对Combretastatin A-4的B环进行结构改造,合成新型的4’-乙氧基Combretastatin A-4。以溴化三甲氧基苄基三苯基鏻与乙氧基异香兰素为原料,经基团保护、缩合、脱保护等反应合成4’-乙氧基Combretastatin A-4。目标化合物经核磁共振氢谱、熔点等确证其化学结构,总收率均达到62%左右。该路线反应条件简便,步骤较短,对顺式产物选择性高。
對Combretastatin A-4的B環進行結構改造,閤成新型的4’-乙氧基Combretastatin A-4。以溴化三甲氧基芐基三苯基鏻與乙氧基異香蘭素為原料,經基糰保護、縮閤、脫保護等反應閤成4’-乙氧基Combretastatin A-4。目標化閤物經覈磁共振氫譜、鎔點等確證其化學結構,總收率均達到62%左右。該路線反應條件簡便,步驟較短,對順式產物選擇性高。
대Combretastatin A-4적B배진행결구개조,합성신형적4’-을양기Combretastatin A-4。이추화삼갑양기변기삼분기린여을양기이향란소위원료,경기단보호、축합、탈보호등반응합성4’-을양기Combretastatin A-4。목표화합물경핵자공진경보、용점등학증기화학결구,총수솔균체도62%좌우。해로선반응조건간편,보취교단,대순식산물선택성고。
Design and synthesis of a novel Combertastatin A-4 analogue were carried out.Based on the synthesis of Combretastatin A-4,3,4,5-trimethoxybenzyltriphenylphosphonium and ethyoxyisovanilline were used as starting materials vis Wittig reaction to prepare 4＇-ethyoxycombretastatin A-4.The structures of target compounds were confirmed by 1H NMR and melting point.The overall yields were about 62%.The synthetic routes developed herein required simple reaction conditions and few steps,and yield high stereoselectivity of cis-conformation.
