Pharmaessentia Corporation

Chungsun Chien

Ko-Chung Lin

Pin-Shu Chien

Chan-Kou Hwang

This invention relates to a process of synthesizing a &#x3b2;-nucleoside compound of formula (I): wherein Ris alkyl, aryl, cycloalkyl, heteroaryl, or heterocycloalkyl. The process includes reacting a compound of formula (II): with a compound of formula (III): wherein Ris as defined above and X is chloride, bromide, iodide, methanesulfonate, triflate, p-toluenesulfonate, trifluoroacetate, 4-nitrophenoxy, or N-succinimidyloxy, in a solvent and in the presence of a base.

Synthesis of 5-deoxy-5'-fluorocytidine compounds

A process of stereoselectively synthesizing &#x3b2;-nucleoside, e.g., 2'-deoxy-2,2&#x2032;-difluorocytidine, is described. The process includes reacting a tetrahydrofuran compound of the following formula: in which wherein R, R, R, R, and L as defined in the specification, with a nucleobase derivative in the presence of an oxidizing agent.

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Taoyuan County, Taiwan

Chungsun Chien