摘要
以4-(2-溴乙酰基)-α,α-二甲基苯乙酸乙酯(2)为起始原料,先在酸性还原体系中还原,得到亚甲基还原产物(3)再与2-(哌啶-4-烷基)-1H-苯并咪唑(4)在有机碱的作用下进行缩合,然后在无水条件下使用氢化钠拔氢后与氯代乙基乙基醚(6)缩合得到(7),最后,将酯基水解得到2-[4-[2-[4-[1-(2-乙氧基)苯并咪唑-2-基]哌啶-1-基]乙基]苯基]-2-甲基丙酸(比拉斯汀,1)。
Bilastin was prepare from 4-(2-bromoacetyl group)--α,α-ethyl dimethyl phenylacetate,the methylene reduction product(3)was obtained by reducing in an acid reduction system.Then it was condensed with 2-(piperidine-4-alkyl)-1H-benzimidazole under the action of organic base.Then in the anhydrous condition after using sodium hydride to draw hydrogen and chloroethyl ethyl ether(6)condensation to get(7),Finally,the ester group was hydrolyzed to obtain 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid(Bilastin,1).
作者
钟雪彬
王晓
王正泽
林辉
Zhong Xuebin;Wang Xiao;Wang Zhengze;Lin Hui(Nanjing Changao Pharmaceutical Technology Limited,Nanjing210000,China)
出处
《山东化工》
CAS
2020年第17期49-50,共2页
Shandong Chemical Industry
关键词
比拉斯汀
新型第2代组胺H1受体拮抗剂
合成
Bilastin
A novel second generation histamine H1 receptor antagonist
synthesis
