REGIOSPECIFIC SYNTHESIS OF RAPAMYCIN 42-ESTER DERIVATIVES Russian patent published in 2010 - IPC C07D498/18 C12P17/18 A61K47/48 A61P35/00 

Abstract RU 2387657 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a method for regiospecific synthesis of rapamycin 42-ester derivatives of formula , where R is ketal isopropylidene substituted with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid, linear or branched C1-C10 alkyl, which possibly contains a halogen, C2-C8 alkenyl, or phenyl, where the said method involves acylation of 42-hydroxyrapamycin with an acyl donor in the presence of lipase. The invention also relates to regiospecific preparation of rapamycin 42-ester from ketal isopropylidene substituted with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid in the presence of lipase.

EFFECT: increased output of the product under mild conditions.

13 cl, 12 ex

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RU 2 387 657 C2

Authors

Gu Dzhianksin

Kaj Ping

Ruppen Mark E.

Dates

2010-04-27Published

2005-04-12Filed