阿替美唑盐酸盐合成工艺的改进

Improved Synthesis of Atipamzole Hydrochloride

摘要:

以2-(2-溴乙酰基）-2-乙基茚酮为原料经过咪唑成环，羰基还原两步后盐酸化合成盐酸阿替美唑。改进了咪唑成环过程工艺条件，并考察了反应温度对收率的影响，确定了最佳反应条件，将咪唑成环反应的收率提高至72％。对于羰基还原过程采用黄鸣龙还原法替代原有的钯碳还原法，采用正交实验法优化了反应条件，确定了最优的工艺条件。

Abstract:

Atipamzole Hydrochloride was synthesized from 2 - (2 - bromine acetyl) - 2 - ethylindanone through three-step reations includingthe imidazole ring formation, carbonyl reduction and hydrochloric acid .The technological conditions of imidazole ring formation were improved, and the effect of reaction temperature on the yield was investigated, Determined the optimum reaction conditions .The yield of the reaction was increased to 72%. In the process of reduction of the carbonyl group, the method of Huang Minglong reduction was used to replace the original palladium carbon reduction method, and the reaction conditions were optimized by orthogonal experiment. The optimum technological conditions were determined