摘要
本文分别以L-苯丙氨酸甲酯盐酸盐和叔丁氧羰基保护的L-苯丙氨酸为起始原料,经两种不同的合成路线,完成了Boc-L-(苯丙)噻唑-4-甲酸甲酯的合成。其中,第一条路线共五步反应,总收率18%;第二条路线共四步反应,总收率22%,两条路线所涉及的官能团转换和反应有:氨基Boc保护、酯基还原、羟基Parikh-Doering氧化,MnO_2氧化,N-甲氧基-N-甲酰胺化。
Two different synthetic routes had been developed for the synthesis of Boc-L-（ Phe）Thz-OMe from L-phenylalanine methyl ester or A^-（tert-Butyloxycarbonyl） -L-phenylalanine,respectively. The first route consisted of five steps and gave 18%total yield;the second route consisted of four steps and gave 22% total yield. The key transformations include Boc protection, methyl ester reduc-tion, Parikh-Doering oxidation, manganese dioxide dehydrogenation and A^-formylation of O-methylhydroxylamine.
出处
《化学研究与应用》
CAS
CSCD
北大核心
2017年第4期542-546,共5页
Chemical Research and Application
基金
河北省自然科学基金项目(B2015208314)资助
