Union Quimico-farmaceutica S.a.

Antonio Domingo Coto

Alexander Christian Comely

Llorenç Rafecas Jané

Xavier Verdaguer Espaulella

Francesc Xavier Verdaguer Espaulella

Llorenç Rafecas Jane

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 &#x2014;(CH)&#x2014;OH group or a &#x2014;(CH)-0-(CH)&#x2014;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), 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 &#x2014;CH)-0-(CH)&#x2014;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. 

[object Object]

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.

Growing community of inventors

Barcelona, Spain

Antonio Domingo Coto