摘要
以3-苯甲酰丙烯酸乙酯(BZ)和三氟乙酰赖氨酸(LA1)为原料,在三氟甲磺酸三正丁胺盐催化作用下,经迈克尔加成反应、氢化还原反应合成赖诺普利关键中间体N2-(1-乙氧羰基-3-苯丙基)-N6-三氟乙酰基-L-赖氨酸(LA2),总收率为38.8%。LA2加成物立体选择性可达到84:16。该方法具有操作简单,收率高,是一条适合工业化生产的合成路线。
The （R）-2-（（R）- 1-ethoxy- 1--oxo-4-phenylbutan-2-ylamino）-6-（2,2,2-trifluoroaeetamido）hexanoic acid （LA2） was obtained by Michael addition from 3-benzoyl ethyl acrylate with （S）-2-amino--6-（2,2, 2- trifluoroacetamido） hexanoic acid in the presence of tributylamine triflate, followed by reduction with Pd/C. The ratio of S-LA/R-LA2 can reach 84：16, and the total yield is 38.8%. This synthetic route is suitable for large scale manufacture.
出处
《浙江化工》
CAS
2012年第9期15-17,6,共4页
Zhejiang Chemical Industry
