PROCESS FOR THE SYNTHESIS OF CMHTP AND INTERMEDIATES THEREOF

摘要

The present invention provides 3-benzyloxy-2-aminopyridine (BOPA), 3-(2- Hydroxyethyl)-2-methyl-9-hydoxy-4H-pyrido[ 1,2-a]pyrimidine-4-one (HMBP), 3-(2- Chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and 3- (2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[l,2-a]- pyrimidin- 4-one (CMHTP) useful as intermediates for the preparation of paliperidone. The present invention also provides processes for preparing these intermediates and for preparing paliperidone.