发明授权
US07678902B2 Process for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)dibenzo[b,f][1,4]thiazepine
失效
制备11-(4- [2-(2-羟基乙氧基)乙基] -1-哌嗪基)二苯并[b,f] [1,4]硫氮杂
- 专利标题: Process for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)dibenzo[b,f][1,4]thiazepine
- 专利标题(中): 制备11-(4- [2-(2-羟基乙氧基)乙基] -1-哌嗪基)二苯并[b,f] [1,4]硫氮杂
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申请号: US11571116申请日: 2005-06-17
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公开(公告)号: US07678902B2公开(公告)日: 2010-03-16
- 发明人: Byong-Sung Kwak , Sang-Il Lee , Hee-Jun Hwang , Jong-Ho Lim
- 申请人: Byong-Sung Kwak , Sang-Il Lee , Hee-Jun Hwang , Jong-Ho Lim
- 申请人地址: KR Seoul
- 专利权人: SK Holdings Co., Ltd.
- 当前专利权人: SK Holdings Co., Ltd.
- 当前专利权人地址: KR Seoul
- 代理机构: Darby & Darby PC
- 优先权: KR10-2004-0047128 20040623
- 国际申请: PCT/KR2005/001866 WO 20050617
- 国际公布: WO2006/001619 WO 20060105
- 主分类号: C07D417/04
- IPC分类号: C07D417/04
摘要:
Disclosed is a process for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine. In the process, low-priced 2,2′-dithiosalicylic acid as starting material is subjected to bond formation reaction with 1-chloro-2-nitrobenzene in a basic aqueous solution, a nitro group reduction reaction is conducted, cyclization and chlorination reactions are simultaneously carried out in the presence of a equivalent amount of halogenating agent, a reaction with piperazine is continuously conducted without separation, and a reaction with 2-haloethoxyethanol is conducted, thereby it is possible to economically producing Quetiapine, that is, 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine, in an environmentally friendly manner. Particularly, the process is advantageous in that economic efficiency is assured because of use of the low-priced starting material, use of an organic solvent is minimized because a reaction is conducted in an aqueous solution, and it is possible to achieve the environmentally friendly and economical process having high commercial usefulness because the number of reaction steps of the process is reduced and because generation of acidic waste is minimized.