|本期目录/Table of Contents|

[1]郭希,杨艺虹*,张珩,等.5(2氯乙酰基)6氯吲哚酮的合成[J].武汉工程大学学报,2010,(11):25-27.[doi:10.3969/j.issn.16742869.2010.11.007]
　GUO Xi,YANG Yi hong,ZHANG Heng,et al.Study on synthesis of 5(2chloroacetyl)6chloroindolinone[J].Journal of Wuhan Institute of Technology,2010,(11):25-27.[doi:10.3969/j.issn.16742869.2010.11.007]
点击复制

5(2氯乙酰基)6氯吲哚酮的合成(/HTML)
分享到：

《武汉工程大学学报》[ISSN:1674-2869/CN:42-1779/TQ]

卷:
期数:
2010年11期
页码:
25-27
栏目:
化学与化学工程
出版日期:
2010-11-30

文章信息/Info

Title:
Study on synthesis of 5(2chloroacetyl)6chloroindolinone
文章编号:
16742869(2010)11002503
作者:
郭希; 杨艺虹*; 张珩; 杨建设; 刘星星
武汉工程大学,湖北省新型反应器与绿色化工工艺重点实验室,湖北 武汉 430074
Author(s):
GUO Xi;  YANG Yihong;  ZHANG Heng;  YANG Jianshe;  LIU Xingxing
Key Laboratory for Green Chemical Process of Ministry of Education,
School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430074,China
关键词:
对氯邻硝基甲苯; 5(2氯乙酰基)6氯吲哚酮; 合成
Keywords:
5(2chloroacetyl)6chloroindolinone; 4chloro1methyl2nitrobenzene; synthesis
分类号:
TQ463+.4
DOI:
10.3969/j.issn.16742869.2010.11.007
文献标志码:
A
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.
Abstract:
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.

参考文献/References:

［1］王海.非典型抗精神病药物的研究进展［J］.河北医科大学学报,2006,27(1):5962.
［2］Charles, Caley F, Chandra, et al.Ziprasidone: the fif thatypical antipsychotic［J］.Ann Pharmacother,2002,36:839.
［3］梁海霞,李焕德.抗精神病新药齐拉西酮的药物动力学研究概况［J］.中南药学,2007,5(3):4549.
［4］王鹏,李海华.由邻硝基甲苯制备邻卤苯乙酸的新方法［J］.北京理工大学学报,2000,20(2):254256.
［5］Protiva M, Sedivy Z, Metysova J. 6Hydroxy10(4methylpiperazino)10,11dihydrodibenzo ［b,f］thiepin and its derivatives［J］. Collect Czechoslovak Chem Commun,1975,40(9):26672675.
［6］张杰,魏安强,骆有寿.2,2 二硝基联苄的铁粉还原新工艺研究［J］.化学世界,2000(5):245.
［7］罗先金,修乃云,阎建民.含卤素取代基中间体的还原工艺［J］.化学工业与工程,2008,25(1):994.
［8］Harada K, Nishino S, Hirotsu K, et al. Process for producing 5fluorooxyindole and for producing intermediate therefore: WO, 2002006228［P］.2002-01-24.
［9］陈卫东,钱旭红,宋恭华,等.2氨基5氟苯甲酸的制备方法:CN,0303129637.8［P］.2004-02-25.
［10］Benages I A, Albonieo S M. Chloroacrylonitrile as a cydodipo larophile in cyeloadditions eyanopyrroles［J］. J Org Chem,1978,43:42724273.
［11］蔡可迎.氧化吲哚合成方法的改进［J］.精细石油化工进展,2006,7(5):2627.
［12］张涛,范江,朗方,等.西洛多辛关键中间体合成工艺改进［J］.四川大学学报:自然科学版,2007,44(3):638640.
［13］史大昕,冯亚青,李倩.4氨基邻苯二甲酰亚胺的合成研究［J］.精细石油化工进展,2003,4(3):18.

相似文献/References:

备注/Memo

备注/Memo:
张瑞收稿日期：20100607作者简介：郭希(1986)，男，湖北武汉人，硕士研究生.研究方向：药物合成.指导老师：杨艺虹，女，教授，硕士研究生导师.研究方向：药物合成.
更新日期/Last Update: