PROCESS FOR THE SYNTHESIS OF CMHTP AND INTERMEDIATES THEREOF

The present invention provides processes of preparing 3-(2-chloroethyl)- 6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[ 1,2-a]- pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone, wherein the processes use 3-(2-chloroethyl)-2-methyl-9-benzyloxy-4H-pyrido[ 1,2-a]py...

Full description

Saved in:
Bibliographic Details
Main Authors DOLITZKY, BEN-ZION, LANCRY, ELI, SHAPIRO, EVGENY, INI, SANTIAGO, SHMUELY, YARON, PILARSKY, GIDEON
Format Patent
LanguageEnglish
French
Published 28.05.2009
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Online AccessGet full text

Cover

More Information
Summary:The present invention provides processes of preparing 3-(2-chloroethyl)- 6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[ 1,2-a]- pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone, wherein the processes use 3-(2-chloroethyl)-2-methyl-9-benzyloxy-4H-pyrido[ 1,2-a]pyrimidine-4- one (CMBP) and/or 3-(2-chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[l,2- a]pyrimidine-4-one (CMHP) having phosphorus at least partially removed as the intermediate. La présente invention concerne des procédés de préparation de 3-(2-chloroéthyl)-6,7,8,9-tétrahydro-9-hydroxy-2-méthyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (CMHTP) utile comme produits intermédiaires pour la préparation de palipéridone, ces procédés consistant à utiliser une 3-(2-chloroéthyl)-2-méthyl-9-benzyloxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMBP) et/ou une 3-(2-chloroéthyl)-2-méthyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) dont le phosphore a été au moins partiellement enlevé comme produit intermédiaire.
Bibliography:Application Number: WO2008US02652