Abstract: A process for the preparation of an 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine derivative, of general Formula (I), where A is hydrogen or a —(CH2)2—OH group or a —(CH2)2-0-(CH2)2—OH group, or of a salt thereof, comprises a step in which 10H-dibenzo[b,f][1,4]thiazepin-11-one is reacted with a piperazine derivative in the presence of a titanium alkoxide of general formula Ti(OR)4, where R is a straight or branched alkyl group, having from one to eight carbon atoms to obtain said Formula I derivative or a salt thereof. Where A is —CH2)2-0-(CH2)2—OH, then the piperazine derivative is 1-(2-(2-hydroxyethoxy)ethyl)piperazine and the 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine is quetiapine, (11-(4-(2-(2-hydroxyethoxy)ethyl)-1-piperazinyl)dibenzo[b,f][1,4]thiazepine). The process may comprise an additional step of reacting the quetiapine with fumaric acid to obtain quetiapine hemifumarate.
Type:
Grant
Filed:
December 21, 2005
Date of Patent:
March 8, 2011
Assignee:
Union Quimico-Farmaceutica S.A.
Inventors:
Alexander Christian Comely, Francesc Xavier Verdaguer Espaulella, Llorenç Rafecas Jané, Antonio Domingo Coto
Abstract: A process for the preparation of (S)-omeprazole from racemic omeprazole via the formation of an inclusion complex with (S)-1,1,2-triphenyl-1,2-ethanediol. (S)-Omeprazole is recovered in a substantially optically pure form either in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. The (S)-omeprazole 2[(S)-1,1,2-triphenyl-1,2-ethanediol] inclusion complex is new. This resolution process proceeds with high yields and high optical purity.
Type:
Grant
Filed:
December 18, 2006
Date of Patent:
September 21, 2010
Assignee:
Unión Químico Farmacéutica, S.A.
Inventors:
Antonio Domingo Coto, Alexander Comely, Xavier Verdaguer Espaulella, Llorenç Rafecas Jané
Abstract: A process for the preparation of (S)-omeprazole from racemic omeprazole via the formation of an inclusion complex with (S)-1,1,2-triphenyl-1,2-ethanediol. (S)-Omeprazole is recovered in a substantially optically pure form either in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. The (S)-omeprazole 2[(S)-1,1,2-triphenyl-1,2-ethanediol] inclusion complex is new. This resolution process proceeds with high yields and high optical purity.
Type:
Application
Filed:
December 18, 2006
Publication date:
December 4, 2008
Applicant:
UNION QUIMICO FARMACEUTICA, S.A.
Inventors:
Antonio Domingo Coto, Alexander Comely, Xavier Verdaguer Espaulella, Llorenc Rafecas Jane