Invention Grant
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
- Patent Title: Process for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)dibenzo[b,f][1,4]thiazepine
- Patent Title (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
-
Application No.: US11571116Application Date: 2005-06-17
-
Publication No.: US07678902B2Publication Date: 2010-03-16
- Inventor: Byong-Sung Kwak , Sang-Il Lee , Hee-Jun Hwang , Jong-Ho Lim
- Applicant: Byong-Sung Kwak , Sang-Il Lee , Hee-Jun Hwang , Jong-Ho Lim
- Applicant Address: KR Seoul
- Assignee: SK Holdings Co., Ltd.
- Current Assignee: SK Holdings Co., Ltd.
- Current Assignee Address: KR Seoul
- Agency: Darby & Darby PC
- Priority: KR10-2004-0047128 20040623
- International Application: PCT/KR2005/001866 WO 20050617
- International Announcement: WO2006/001619 WO 20060105
- Main IPC: C07D417/04
- IPC: C07D417/04
![Process for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)dibenzo[b,f][1,4]thiazepine](/abs-image/US/2010/03/16/US07678902B2/abs.jpg.150x150.jpg)
Abstract:
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.
Public/Granted literature
Information query