PROCESSO DE PREPARACAO DE UM COMPOSTO ACTIVO SOB O PONTO DE VISTA FARMACEUTICO (GRANISETRON)

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 0-100° C., in the presence of a strong acid, in order to yield the compound of fo...

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Bibliographische Detailangaben
Hauptverfasser: PERE DALMASES BARJOAN, TORRES, SALVADOR PUIG
Format: Patent
Sprache:por
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Beschreibung
Zusammenfassung: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 0-100° 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° C.-160° 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.