Process for producing erythromycin derivative

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

Reexamination Certificate

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C536S018500

Reexamination Certificate

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06897299

ABSTRACT:
A method for preparing a fumarate salt of a compound represented by Formula (II):(wherein R1represents a hydrogen atom or a lower alkyl group, and R2represents a lower alkyl group), which comprises carbamating a compound represented by Formula (I):(wherein R1represents 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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patent: 5959088 (1999-09-01), Miura et al.
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patent: 0215355 (1987-03-01), None
patent: 0846697 (1998-06-01), None
patent: 01-203398 (1989-08-01), None
Tadanier, et al.Some Chemical and Stereochemical Modifications of the Erythromycin Lactone Rings, Journal of Organic Chemistry, vol. 39, No. 17 (1974), pp. 2495-2501.

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