Chugai Seiyaku Kabushiki Kaisha

Mitsuhiro Kurita

Hitoshi Shimizu

Kaname Tsuzaki

A method for preparing a fumarate salt of a compound represented by Formula (II):(wherein Rrepresents a hydrogen atom or a lower alkyl group, and Rrepresents a lower alkyl group), which comprises carbamating a compound represented by Formula (I):(wherein Rrepresents 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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Tokyo, Japan

Mitsuhiro Kurita