洛匹那韦合成工艺研究

Synthesis of lopinavir

目的洛匹那韦合成工艺的优选。方法以(2S,3S,5S)-2-胺基-3-羟基-5-(叔丁氧羰基胺基)-1,6-二苯基己烷的丁二酸盐为原料,经酰胺化、氨基脱保护、酰胺化三步反应制备洛匹那韦。结果较高收率合成了高纯度的洛匹那韦(纯度>99%;总产率70%)。结论得到了简洁、绿色、适于工业化生产的洛匹那韦制备工艺。

Abstrast ：Objective To optimize the synthesis of lopinavir. Methods Lopinavir was synthesized via three steps including amidation, deprotection of amine, and amidation from （ 2 S, 3 S, 5 S ） -2 -amino-3 -hydroxy-5 - （ tert-butoxycarbonyl- amino ） - 1,6 -diphenyl hexane sue cinate. Results Lopinavir was synthesized with high yield and purity （ purity 〉 99% ： overall yield 70% ）. Conclusions A simple, green, suitable preparation process for industrial production of lopinavir was got.