A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/495 (2006.01) A61K 31/00 (2006.01) A61K 31/50 (2006.01) C07D 401/12 (2006.01)
Patent
CA 2495659
This invention describes a process for preparing hydroxyazapirones of Formula (I) from azapirones of Formula (II). The process comprises treating azapirones with a strong base, monitoring enolate formation of the azapirone by IR spectroscopy, and reacting the enolate with a source of molecular oxygen in the presence of a reductant. The process is suitable for large scale production of hydroxyazapirones.
L'invention concerne un procédé de préparation d'hydroxyazapirones de formule (I) à partir d'azapirones de formules (II). Le procédé consiste à traiter des azapirones avec une base forte, à contrôler la formation d'énolate de l'azapirone par spectroscopie IR, et à faire réagir l'énolate avec une source d'oxygène moléculaire en présence d'un réducteur. Le procédé est approprié pour la production, à grande échelle, d'hydroxyazapirones.
Depue Jeffrey
Dowdy Eric D.
Kotnis Atul S.
Leung Simon
Watson Daniel J.
Bristol-Myers Squibb Company
Gowling Lafleur Henderson Llp
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