Esteve Quimica S.a.

Inke, S.a.

Laboratorios Vita, S.a.

Salvador Puig Torres

Marti Bartra Sanmarti

Pere Dalmases Barjoan

Reyes Herbera Espinal

Montserrat Monsalvatje Llagostera

Montserrant Monsalvatje Llagostera

Jaime Tomas Navarro

Jaime Thomas Navarro

The invention relates to a procedure for preparing quetiapine by reaction between a compound of formula (II) and a compound of formula (III), in which X means a leaving group and P a protective group of alcohols resistant to alkaline conditions, in the presence of a base, followed by a step of deprotection and, optionally, obtaining a pharmaceutically acceptable salt thereof. Said procedure permits the obtaining of quetiapine with a high degree of purity under soft temperature conditions, with short reaction times and avoiding the use of toxic solvents. (Graphic) 

Procedure for preparing 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazineyl)-dibenzo[b,f] [1,4]thiazepine

The process for obtaining quinapril hydrochloride (I) comprises the stages of: a) hydrogenolysis of the benzyl ester of quinapril (II) by treatment in an alcoholic solvent, with concentrated hydrochloric acid or a solution of hydrogen chloride in isopropanol, and hydrogenation; b) removal of the solvent; c) addition of toluene to precipitate the quinapril hydrochloride as a toluene solvate; d) treatment of said solvate with a Class 3 solvent which forms a solvate of quinapril hydrochloride from which it can be removed by drying without degrading; and e) drying of the solvate from step d) to yield quinapril hydrochloride (I), an antihypertensive agent.

Process for obtaining quinapryl hydrochloride and solvates useful for isolating and purifying quinapryl hydrochloride

The invention relates to a process for preparing granisetron, or a pharmaceutically acceptable salt thereof, which comprises: a) cyclisation of a compound of formula (I) in an inert solvent and at a temperature between 0&#x2013;100&#xb0; C., in the presence of a strong acid, in order to yield the compound of formula (II); b) methylation of the compound of formula (II), with an alkylating agent, in the presence of a base, in an inert solvent and at a temperature between 0&#xb0; C.&#x2013;160&#xb0; C., and with optional formation of a pharmaceutically acceptable salt. The process of the invention yields a granisetron of high purity, preventing impurities due to demethylation, by carrying out the methylation after rather than before cyclisation and with a higher yield.

Process for preparing a pharmaceutically active compound (granisetron)

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Barcelona, Spain

Salvador Puig Torres