Process for preparing water-soluble polyethylene glycol...

Details Process for preparing water-soluble polyethylene glycol... Process for preparing water-soluble polyethylene glycol...

A - Human Necessities

61

K

A61K 47/48 (2006.01) A61P 37/06 (2006.01)

Patent

CA 2644156

Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the acylated rapamycin with a methoxy poly(ethylene glycol) derivative in the presence of a base. Also described are processes for preparing 32-pegylated tacrolimus and/or ascomycin using these steps.

L'invention concerne des procédés de préparation de rapamycines 42-pégylées, consistant à faire réagir une rapamycine avec un agent acylant en présence d'une lipase afin de former une rapamycine acylée et à faire réagir la rapamycine acylée avec un dérivé de méthoxypolyéthylène glycol en présence d'une base. L'invention concerne également des procédés de préparation de tacrolimus et/ou ascomycine 32-pégylés en suivant les mêmes étapes.

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