GABA_(A)受体激动剂PF0713的合成  

Synthesis of GABA_(A) Receptor Agonist PF0713

作　　者：郝帅帅 郑璐 陈寅 张桂森 吴庆昆 Hao Shuaishuai;Zheng Lu;Chen Yin;Zhang Guisen;Wu Qingkun(Jiangsu Ocean University,School of Pharmacy,Lianyungang,222005)

机构地区：[1]江苏海洋大学药学院,连云港222005

出　　处：《化学通报》2022年第2期264-267,共4页Chemistry

基　　金：江苏省海洋资源开发研究院开放基金项目(JSIMR202015)资助。

摘　　要：2,6-二((R)-仲丁基)苯酚(PF0713)是在丙泊酚的基础上开发的一种新型烷基酚类静脉麻醉类药物。本文以邻仲丁基苯酚和1-氯-2-丁烯为起始原料,经烃化反应、Claisen重排反应和氢化反应以59.2%的收率得到2,6-二仲丁基苯酚,后经手性拆分得到PF0713,其结构经^(1)H NMR、^(13)C NMR和LC-MS确证。2,6-di((R)-sec-butyl)phenol(PF0713)is a new type of alkylphenol intravenous anesthetic developed on the basis of propofol.In this paper,2-sec-butylphenol and 1-chlorobut-2-ene were used as raw materials,and 2,6-di-sec-butylphenol was obtained with the yield of 59.2%by a series of reactions including alkylation,Claisen rearrangement and hydrogenation.Then PF0713 was obtained by chiral resolution.The structures were characterized by ^(1)H NMR,^(13)C NMR and LC-MS.

关 键 词：2 6-二((R)-仲丁基)苯酚 麻醉药 工艺优化 Claisen重排反应 手性拆分 

分 类 号：TQ460.1[化学工程—制药化工]