Applied result detail
Synthesis of paliperidone
Jiri Bartl, Petr Benovsky, Jozef Krajcovic
Original Title
Synthesis of paliperidone
English Title
Synthesis of paliperidone
Type
Patent
Original 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.
English 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
18.06.2009
Owner
SYNTHON B.V. Microweg 22, NL-6545 CM Nijmegen
Licence fee
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