发明名称 |
PROCESS FOR PREPARING QUETIAPINE AND QUETIAPINE FUMARATE |
摘要 |
The invention comprises a process for preparing quetiapine and/or its salts, including, quetiapine fumarate. The process generally comprises reacting dibenzothiazepinone (dibenzo[bf][l,4]thiazepin-l l(10H)-one) with phosphorous oxychloride in the presence of triethylamine in an aromatic organic solvent such as toluene or, preferably, xylene at reflux temperature to obtain an aromatic hydrocarbon solution of 11-chloro-dibenzo [bf] [1,4] thiazepine. Thereafter, the l l-chloro-dibenzo[bf][1,4] thiazepine is reacted with 2-(2-piperazin-l-ylethoxy)-ethanol to yield, following several processing steps, quetiapine.. Compound I can then be further reacted with fumaric acid at elevated temperature to yield quetiapine fumarate. The resulting quetiapine fumarate obtained is suitable for use in pharmaceutical preparations. |
申请公布号 |
WO2006117700(A3) |
申请公布日期 |
2007.03.01 |
申请号 |
WO2006IB02286 |
申请日期 |
2006.04.21 |
申请人 |
MEDICHEM, S.A.;BOSCH LLADO, JORDI;BURGAROLAS MONTERO, MARIA CARMEN;CHAMORRO GUTIERREZ, IOLANDA |
发明人 |
BOSCH LLADO, JORDI;BURGAROLAS MONTERO, MARIA CARMEN;CHAMORRO GUTIERREZ, IOLANDA |
分类号 |
C07D281/16;A61K9/14;A61K31/554;A61P25/08 |
主分类号 |
C07D281/16 |
代理机构 |
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