| 齐拉西酮的合成 |
| |
| 引用本文： | 王怡,张珩,杨艺虹,王琛.齐拉西酮的合成[J].精细化工中间体,2010,40(5):37-39,42. |
| |
| 作者姓名： | 王怡 张珩 杨艺虹 王琛 |
| |
| 作者单位： | 武汉工程大学绿色化工过程省部共建教育部重点实验室,湖北武汉430073 |
| |
| 摘 要： | 以3-氯-1,2-苯并异噻唑和无水哌嗪为原料合成1-(1,2-苯并异噻唑-3-基)哌嗪(2),以6-氯-1,3-二氢-吲哚酮和氯乙酰氯为原料经Friedel-crafts酰化制备5-(2-氯乙酰基)-6-氯-1,3-二氢-吲哚酮(3),3经硼氢化钠和三氟乙酸还原制得5-(2-氯乙基)-6-氯-1,3-二氢-吲哚酮(4),2和4在碘化钠/碳酸钠的水溶液中缩合得到齐拉西酮(1),总收率50.5%(以3-氯-1,2-苯并异噻唑计,n/n)。齐拉西酮的结构经IR和1H NMR确证。
|
| 关 键 词： | 抗精神病药 齐拉西酮 Friedel-crafts酰化 合成 |
Synthesis of Ziprasidone |
| |
| WANG Yi,ZHANG Heng,YANG Yi-hong,WANG Chen.Synthesis of Ziprasidone[J].Fine Chemical Intermediates,2010,40(5):37-39,42. |
| |
| Authors: | WANG Yi ZHANG Heng YANG Yi-hong WANG Chen |
| |
| Affiliation: | (Key Laboratory for Green Chemical Process of Ministry of Education,Wuhan Institute of Technology,Wuhan 430073,China) |
| |
| Abstract: | 1,2-Benzoisothiazole-3-piperazine（2） was synthesized from 3-chloro-1,2-benzoisothiazole and piperazine.5-（2-Chloroacetyl）-6-chloro-indole ketone（3） was synthesized from 6-chloro-indole ketone and chloroacetyl chloride by Friedel-crafts acylation.Reduction of 3 by sodium borohydride gave 5-（2-chloroethyl）-6-chloro-indole ketone（4）.Combination of 2 and 4 in aqueous solution of NaI / NaCO3 produced ziprasidone（1） in overall yield of 50.5%.The structures were confirmed by IR and 1H NMR. |
| |
| Keywords: | antipsychotic drug ziprasidone Friedel-crafts acylation synthesis |
| 本文献已被 CNKI 维普 万方数据 等数据库收录！ |
|
