Lipase mediated hydrolysis of rapamycin 42-hemisuccinate benzyl and methyl esters

Abstract

Benzyl and methyl esters of rapamycin 42-hemisuccinate were hydrolyzed under very mild conditions to the rapamycin hemisuccinate using lipase from Pseudomonas sp. This selective deprotection was performed on a ≥100 mg scale for both esters resulting in 50% isolated yield from the methyl ester and 29% from the benzyl ester of the desired acid. © 1994.