摘要
设计了一条齐拉西酮的关键中间体5-(2-氯乙酰基)6-氯-吲哚酮(Ⅰ)的合成路线.以对氯邻硝基甲苯(Ⅱ)和草酸二乙酯为起始原料,经缩合、水解、氧化、脱羰、还原、环合和Friedel-Crafts酰化反应合成得到Ⅰ.产品含量达99%(GC),总收率为34.8%,Ⅰ的结构经1H NMR和IR确证.
We design a route of synthesizing 5-（2-chloroacetyl）-6-chloro-indolinone（Ⅰ）,which is a critical intermediate in the process of synthesis of Ziprasidone.The compound（Ⅰ） was obtained by using 4-chloro-1-methyl-2-nitro-benzene and diethyl ethaneioate as primary materials,followed by condensation,hydrolysis,oxidation,decarbonization,reduction,cyclization and Friedel-Grafts acylation.The overall yield of the product was 34.8% as well as its purity attained 99%.The structure of the compound（Ⅰ） was characterised by 1H-NMR and IR.
出处
《武汉工程大学学报》
CAS
2010年第11期25-27,共3页
Journal of Wuhan Institute of Technology
