Scalable process for the preparation of a rapamycin 42-ester...

C - Chemistry – Metallurgy – 07 – D

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C07D 498/18 (2006.01)

Patent

CA 2630645

A scalable process for the preparation of a rapamycin 42-ester by reacting a rapamycin 42-ester boronate with a diol and purifying crude rapamycin 42-ester by recrystallization and treatment with a diol is provided. Also provided is a method for isolating and purifying a rapamycin 42-ester boronate from mother liquors comprising acetone and rapamycin contaminants.

La présente invention concerne un procédé évolutif pour la préparation d'un 42-ester de rapamycine en faisant réagir un borate de 42-ester de rapamycine avec un diol et en purifiant 42-ester de rapamycine brut par recristallisation et traitement avec un diol. La présente invention concerne en outre un procédé pour isoler et purifier un borate de 42-ester de rapamycine à partir de liqueurs mères comprenant de l'acétone et des contaminants de rapamycine.

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