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乌拉地尔的有效制备
Effective Preparation of Urapidil

DOI: 10.12677/HJMCe.2022.103028, PP. 275-286

Keywords: 乌拉地尔,氨基尿嘧啶,降压药,工艺流程
Urapidil
, Aminouracil, Antihypertensive Drug, Synthesis Process

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Abstract:

本文介绍一种盐酸乌拉地尔的有效工业合成法。乌拉地尔是临床常用的一种降压药物,合成研究已被多个研究团队报道。本团队采用氨基尿嘧啶为起始原料,经胺胺交换、氯代、亲核取代、盐酸成盐、重结晶共5步得到盐酸乌拉地尔,总收率达48.94%,纯度99.9%以上。本文详细阐述了合成盐酸乌拉地尔的工艺流程,为今后工业生产提供准确详实的参考。
This paper introduces an efficient industrial synthesis method of urapidil hydrochloride. Urapidil is a commonly used antihypertensive drug in clinic, and its synthesis research has been reported by several research teams. Our team used aminouracil as the starting material, and obtained urapidil hydrochloride through 5 steps of amine-amine exchange, chlorination, nucleophilic substitution, hydrochloric acid salt formation, and recrystallization, the total yield is 48.94%, and the purity is above 99.9%. This paper expounds the technological process of synthesizing urapidil hydrochloride in detail, and provides accurate and detailed reference for future industrial production.

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