局部麻醉药盐酸达克罗宁高效合成工艺

Synthesis of local anesthetic dyclonine hydrochloride

以对羟基苯乙酮和溴丁烷为起始原料,利用相转移催化剂通过两步反应合成药用级的盐酸达克罗宁。首先利用相转移催化剂催化生成中间体对丁氧基苯乙酮,再与哌啶盐酸盐、多聚甲醛反应生成产物。合成产物经1H-NMR和MS结构确证。结果表明,该反应总产率超过90%,简单易操作,适合工业生产。

Dyclonine hydrochloride is commonly used as local anesthetics. We developed an efficient synthesis process of dyclonine hydrochloride,namely a novel two-step synthesis process. In this process,4-hydroxyacetophenone and n-butyl bromide were used as the starting material,the intermediate 1-（ 4-butoxyphenyl）-ethanone was produced by using the phase-transfer catalyst, and then dyclonine hydrochloride was obtained by further reacting with piperidinium chloride and paraformaldehyde. The structures of dyclonine hydrochloride were confirmed by1H-NMR and MS. The overall yield was more than 90%. It is an easy operation process and suitable for industrial production.