4.8 Article

Lipase-catalyzed regioselective esterification of rapamycin: Synthesis of temsirolimus (CCI-779)

Journal

ORGANIC LETTERS
Volume 7, Issue 18, Pages 3945-3948

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol0514395

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A lipase-catalyzed acylation of the immunosuppressant rapamycin with complete regioselectivity is described. The method was successfully applied to the synthesis of 42-hemiesters and temsirolimus (CCI-779), an investigational oncology drug.

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