贝达喹啉中间体3-苄基-6-溴-2-甲氧基喹啉的合成工艺优化

Optimization of synthetic process of 3-benzyl-6-bromo-2-methoxyquinoline

贝达喹啉是本世纪初开发上市的新型二芳基喹啉类药物,而3-苄基-6-溴-2-甲氧基喹啉是合成贝达喹啉的重要中间体。本文针对此中间体合成时间长,收率低的问题,通过探讨不同的反应时间、温度、溶剂等因素对其影响,寻找到较优的反应条件,提高了反应收率,缩短了反应时间,便于工业化生产。

Beidaquiline is a novel diaryl quinoline drug developed and marketed at the beginning of this century,and 3-benzyl-6-bromo-2-methoxyquinoline is an important intermediate for the synthesis of bedaquiline.This article aimed at the problem of long synthesis time and low yield of this intermediate.Through the discussion of different reaction time,temperature,solvent and other factors,it found better reaction conditions,improved the reaction yield and shortened the reaction time.This condition facilitated industrial production.