Pharmaessentia Corporation

Wensen Li

Ko-Chung Lin

Wei-Der Lee

Chi-Yuan Chu

Chan Kou Hwang

This invention relates to a process of stereoselectively synthesizing a &#x3b2;-nucleoside compound of formula (I): wherein R, R, and B are as defined in the specification; each of Rand R, independently, is H or fluoro. The process includes reacting, in the presence of a transition metal salt, a tetrahydrofuran compound of formula (II): wherein R, R, and L are as defined in the specification, with a nucleobase derivative; and each of Rand R, independently, is H or fluoro.

Synthesis of &#x3b2;-nucleosides

This invention relates to a process for stereoselectively preparing a nucleoside of the following formula: wherein R, R, and B are defined herein. The process includes reacting a furanose compound with a nucleobase in the presence of a halide salt. Also disclosed is another process for stereoselectively synthesizing an intermediate that can be used to make the starting compound in the first-mentioned process.

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Holmdal, NJ, United States of America

Wensen Li