Patent detail

Synthesis of paliperidone

Jiri Bartl, Petr Benovsky, Jozef Krajcovic

Patent type

Patent

Abstract

A 9-hydroxy or 9-acyloxy group can be added to a pyridopyrimidinone ring structure by a process comprising acylating a compound of formula (5) under Vilsmeier-Haack or Friedel-Crafts conditions to form a compound (6); and transforming with a peroxo-compound to obtain the compound (I). R represents hydrogen or a C1-C20 acyl group. The process is useful in the synthesis of paliperidone and derivatives.

Patent number

WO2009074333A1

Date of application

10. 12. 2008

Date of registration

18. 6. 2009

Publisher

Úřad průmyslového vlastnictví (patentový úřad České republiky)

Owner

SYNTHON B.V. Microweg 22, NL-6545 CM Nijmegen

Possibilities of use

In order to use the result by another entity, it is always necessary to acquire a license

Licence fee

The licensor does not require a license fee for the result