盐酸贝那普利产业化工艺研究

Study on the industrialization of process for benazepril hydrochloride synthesis

目的:探讨盐酸贝那普利产业化工艺。方法:以(R)-2-羟基-4-苯基丁酸乙酯为原料,经过酰化、缩合然后水解成盐制备盐酸贝那普利。结果:成品总收率为37.6%,并且质量检测结果符合中国药典质量标准的要求。并对产业化过程中(R)-a-(4-硝基苯磺酰氧基)-4-苯丁酸乙酯的合成工艺以及成品的精制工艺进行了考察。结论:本工艺收率较高,质量稳定,适于产业化生产。

Objective： To study the industrialization of the process for benazepril hydrochloride synthesis. Methods： Benazepril hydrochloride was prepared by using ethyl （R）-2-hydroxy-4-phenylbutyrate as a raw material, followed by acylation, condensation and hydrolysis to salt. Results： The total yield of the product was 37.6%, and the quality test results met the requirements of the quality standard of Chinese pharmacopoeia. The processes for the synthesis of ethyl （R）-（4-nitrobenzene sulfonyl） -4-phenylbutyrate and the refining of final product were also investigated. Conclusion： The process has high yield, stable quality and suitable for industrial production.