盐酸巴尼地平的合成

Synthesis of Barnidipine Hydrochloride

研究了以碳酸氢铵,间硝基苯甲醛和乙酰乙酸甲酯为原料,经缩合、部分水解,再与(s)-N-苄基-3-羟基吡咯烷经酯化、分步重结晶、成盐得到盐酸巴尼地平的工艺路线。本法操作简单,成本较低,适合于工业化生产。

The barnidipine hydroehloride were prepared via cyclocondensation from m- nitrobenzaldehyde, methyl aeetoaeetate and anmmonium bicarbonate, hydrolysis, esterifieation with optiealiy （S） - N - Benzyl - 3 - py - rrolidinol, reerystallisation and salifieation. The process was simple, the reaction conditions were mild, and suitable for scale - up produetion.