Synthesis of paliperidone

Details Synthesis of paliperidone Synthesis of paliperidone

2011-07-12

2011-07-12

Wilson, James O (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

Reexamination Certificate

active

07977480

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 (1).R represents hydrogen or a C1-C20 acyl group. The process is useful in the synthesis of paliperidone and derivatives.

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A. Horvath et al., “Nitrogen Bridgehead Compounds. Part 30. Vilsmeier-Haack Formylation of 6, 7, 8, 9 Tetrahydro-4H-pyrido [1,2-a] pyrimidin-4-ones” (J. Chem. Soc. Perkin Trans. 1, (1983) pp. 369-377.

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