PROCESS FOR THE SYNTHESIS OF CMHTP, A PALIPERIDONE INTERMEDIATE

The present invention provides a process for 3-(2-chloroethyl)-6,7,8,9- tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]- pyrimidin-4-one (CMHTP), comprising reacting 3-(2- chIoroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and/or 3-(2-chIoroethyi)-2-methyl-9-benzyIoxy-4H-pyrido[1...

Full description

Saved in:
Bibliographic Details
Main Authors INI, SANTIAGO, SHMUELY, YARON
Format Patent
LanguageEnglish
French
Published 22.05.2009
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Online AccessGet full text

Cover

More Information
Summary:The present invention provides a process for 3-(2-chloroethyl)-6,7,8,9- tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]- pyrimidin-4-one (CMHTP), comprising reacting 3-(2- chIoroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and/or 3-(2-chIoroethyi)-2-methyl-9-benzyIoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMBP) with a hydrogen source and at least one hydrogenation catalyst to form CMHTP, wherein the hydrogen source is cyclohexene, cyclohexadiene or ammonium formate, and wherein the ammonium formate is mixed with formic acid, and its conversion to paliperidone. L'invention porte sur un procédé permettant d'obtenir de la 3-(2-chloroéthyl)-6,7,8,9- tétrahydro-9-hydroxy-2-méthyl-4H-pyrrido[1,2-a]- pyrimidin-4-one (CMHTP), et de la transformer en palipéridone.
Bibliography:Application Number: WO2008US11433