盐酸达克罗宁的新合成工艺

A New Synthetic Method of Dyclonine Hydrochloride

本研究报道了一条合成盐酸达克罗宁的新方法。苯酚(2)与1-溴丁烷反应得苯丁醚,与3-氯丙酰氯经傅-克酰化反应生成1-(4-丁氧基苯基)-3-氯丙基-1-酮(6),再和哌啶盐酸盐在三乙胺作用下反应得目标化合物。本合成工艺反应条件温和,操作简单,总收率62%(以2计)。其中,化合物6为未见文献报道的新化合物。

A new method for the synthesis of dyclonine hydrochloride was reported. Phenol （2） reacted with 1-bromobutane to give n-butoxybenzene, which was followed by Friedel-Crafts acylation with 3-chloropropionyl chloride to afford 1-（4-butoxyphenyl）-3-chloropropan-l-one （6）. Then the latter reacted with piperidine hydrochloride in the presence of triethylamine to produce the target compound with an overall yield of 62 % （based on 2）. The reaction conditions of this synthetic process were mild and the operation was simple. In this method, compound 6 is a new compound which has not yet been reported in literature.