Process for producing erythromycin derivative

C - Chemistry – Metallurgy – 07 – H

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C07H 17/08 (2006.01)

Patent

CA 2597514

A method for preparing a fumarate salt of a compound represented by Formula (II): (see formula I) (wherein R1 represents a hydrogen atom or a lower alkyl group, and R2 represents a lower alkyl group), which comprises carbamating a compound represented by Formula (I) : (see formula II) (wherein R1 represents a hydrogen atom or a lower alkyl group), removing all carbamate groups from this compound, alkylating the nitrogen atom at the 3'-position of the desosamine ring in the resulting compound to give the compound represented by Formula (II), and converting this compound into a fumarate salt, wherein the compound represented by Formula (I) is carbamated in the presence of a cyclic ether or a carboxylic ester. This method enables efficient preparation of high-quality erythromycin derivatives.

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