Process for preparing rapamycin 42-esters and fk-506...

Details Process for preparing rapamycin 42-esters and fk-506... Process for preparing rapamycin 42-esters and fk-506...

C - Chemistry, Metallurgy

07

D

C07D 498/18 (2006.01) A61K 47/48 (2006.01) C12P 17/18 (2006.01)

Patent

CA 2562962

Methods for the synthesis of regiospecific rapamycin 42-hemiesters and regiospecific FK506 32-esters with dicarboxylic acids is described. The methods involve catalyzing the reaction between a rapamycin or a FK-506 and a dicarboxylic anhydride or a bifunctional activated ester of dicarboxylic acid with a lipase.

L'invention concerne des procédés pour la synthèse de 42-hémiesters de rapamycine régiospécifiques et de 32-esters de FK-506 régiospécifiques avec des acides carboxyliques : on catalyse la réaction entre rapamycine ou FK-506 et un anhydride dicarboxylique ou un ester bifonctionnel activé d'acide dicarboxylique avec une lipase.

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