Regiospecific synthesis of rapamycin 42-ester derivatives

Details Regiospecific synthesis of rapamycin 42-ester derivatives Regiospecific synthesis of rapamycin 42-ester derivatives

C - Chemistry, Metallurgy

07

D

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

Patent

CA 2562952

A method for the regiospecific synthesis of rapamycin 42-ester derivatives is described. The method involves lipase-catalyzed acylation of 42 hydroxy rapamycin with an acyl donor such as a vinyl ester, an isopropenyl ester or an anhydride in a suitable organic solvent.

L'invention concerne un procédé pour la synthèse régiospécifique de dérivés de 42-esters de rapamycine : acylation catalysée par lipase de 42-hydroxy rapamycine avec un donneur d'acyle du type ester de vinyle, ester d'isopropényle ou anhydride dans un solvant organique approprié.

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