公开(公告)号：EP1817289A1

公开(公告)日：2007-08-15

申请号：EP04798127.9

申请日：2004-11-30

申请人： Medichem, S.A.

发明人： CHAMORRO GUTIERREZ, Iolanda ,  BOSCH I LLADO, Jordi ,  MOLINS I GRAU, Elies

IPC分类号： C07D215/18

CPC分类号： C07D215/18

摘要： The present invention relates to a novel process for the preparation of montelukast sodium, a compound of Formula (1b) and precursors thereof. The invention further concerns the free acid of this compound in crystalline form, obtainable for the first time by the new process.

公开(公告)号：EP1879874A2

公开(公告)日：2008-01-23

申请号：EP06765649.6

申请日：2006-04-21

申请人： Medichem, S.A.

发明人： BOSCH LLADÓ, Jordi ,  BURGAROLAS MONTERO, Maria Carmen ,  CHAMORRO GUTIERREZ, Iolanda

IPC分类号： C07D281/16 ,  A61K31/554 ,  A61K9/14 ,  A61P25/08

CPC分类号： A61K9/2059 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  C07D281/16

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.