摘要
左羟丙哌嗪作为一种国内尚未进口和生产的药物 ,对其合成工艺的研究 ,可为工业生产该种药物打下基本的技术基础。该工艺用苯胺、二乙醇胺在酸性条件下 ,于 2 2 0℃左右环合制得苯基哌嗪 ;环氧氯丙烷用 10 %的硫酸开环成 3-氯 - 1,2 -丙二醇 ;然后将这两种中间体在乙醇溶液中回流 ,制得消旋体羟丙哌嗪 ,再用酒石酸拆分制得左羟丙哌嗪。通过该方法可以制得产品 ,总收率达 9.5 %。并通过结构鉴定 ,确证其为左羟丙哌嗪。
Levodropropizine, a new drug that can not be exported and produced in domestic market, in order to obtain this new drug, we develop the method of synthesizing it. The N_Phenylpiperazine was prepared by mixing aniline and diethanolamine in the presence of Al 2O 3 and concentrated hydrochloric acid. The mixture was heated to 220 ℃. The epichlorohydrin was hydrolyzed to 3 chloro 1,2 propanediol in sulfuric aqueous solution at 80 ℃,and then the dropropizine was obtained by combining the N Phenylpiperazine and 3 chloro 1,2 propanediol. The resolution of dropropizine is carried out by treating it with L (+) tartaric acid in aqueous medium to give Levodropropizine.The levodropropizine can be obtained and produced according to this.
出处
《重庆大学学报（自然科学版）》
EI
CAS
CSCD
北大核心
2002年第3期87-88,共2页
Journal of Chongqing University
