萘普生中间体2-氨基-2-(5-溴-6-甲氧基-2-萘基)丙酸的合成

Synthesis of 2-Amino-2-(5-bromo-6-methoxy-2-naphthyl) Propionic Acid

采用 1,3-二溴 - 5 ,5 -二甲基乙内酰脲作溴化剂 ,在丙酮溶剂中 ,以盐酸作催化剂 ,于室温快速 (8min)、高收率(96 % )地对 2 -甲氧基萘的萘环进行溴化 ,再经乙酰化、Bucherer- Berg环化和水解反应 ,制得萘普生中间体 2 -氨基 -2 - (5 -溴 - 6 -甲氧基 - 2 -萘基 )丙酸。并对环化反应的条件进行了优化 ,反应总收率 6 8%。

Amino 2 (5 bromo 6 methoxy 2 naphthyl) propionic acid, the intermediate of naproxen, was synthesized by bromination of 2 methoxynaphthalene with 1,3 dibromo 5,5 dimethyl hydantoin (DBDMH) in the presence of a catalytic amount of hydrochloric acid in acetone with the yield of 96% within 8 min, acylation, Bucherer Berg's reaction and hydrolysis. The reaction condition of the Bucherer Berg's reaction was optimized. The overall yield was 68%.