Process for the synthesis of azetidinones

Details Process for the synthesis of azetidinones Process for the synthesis of azetidinones

C - Chemistry, Metallurgy

07

D

C07D 205/08 (2006.01)

Patent

CA 2166784

This invention provides a process for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, particularly for azetidinones substituted in the C-3 and C-4 positions and optionally substituted at the ring nitrogen, comprising reacting a .beta.-(substituted-amino)amide, a .beta.-(substituted-amino)acid ester, or a .beta.-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent.

Procédé de préparation d'azétidinones utiles comme intermédiaires de synthèse des pénèmes et comme agents hypocholestrolémiques, notamment en ce qui concerne les azétidinones substituées aux positions C-3 et C-4, et facultativement substituées au niveau de l'azote du cycle. Ledit procédé consiste à faire réagir une beta -amide (amino substituée), un beta -ester d'acide (amino substitué) ou un beta -ester d'acide thiolcarbonique (amino substitué), avec un agent de silylation et un agent de cyclisation.

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