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. 2005 Sep 1;7(18):3945-8.
doi: 10.1021/ol0514395.

lipase-catalyzed regioselective esterification of rapamycin: synthesis of temsirolimus (CCI-779)

Jianxin Gu  1 , Mark E Ruppen, Ping Cai
Affiliations

lipase-catalyzed regioselective esterification of rapamycin: synthesis of temsirolimus (CCI-779)

Jianxin Gu et al. Org Lett. .

Abstract

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.[reaction: see text]

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