Union Quimico-farmaceutica S.a.

Francesc Xavier Verdaguer Espaulella

Alexander Christian Comely

Llorenç Rafecas Jané

Antonio Domingo Coto

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. 

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Vic, Spain

Francesc Xavier Verdaguer Espaulella