Polyene macrolide schiff bases, their alkyl esters and processes

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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514 31, C07H 1704, A61K 3170

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active

059817216

ABSTRACT:
Processes for the preparation of high purity alkyl esters of polyene macrolide antibiotics are disclosed. The processes involve treating an amphoteric polyene macrolide antibiotic with an aldehyde to yield the corresponding Schiff base which is soluble in the reaction medium. The solution is then treated with an alkylating agent in the presence of a hindered tertiary amine as acid acceptor to yield the alkyl ester of the polyene macrolide antibiotic in the form of its Schiff base derivative. Contacting this derivative with water converts the Schiff base derivative to the desired alkyl ester of the polyene macrolide antibiotic which is recovered from the reaction medium.

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