PRODUCTION OF 2'-DEOXY-BETA-CYTIDINE DERIVATIVE AND SALT THEREOF

摘要

PURPOSE:To industrially and readily obtain the subject derivative useful as an antiviral agent, etc., in high yield by subjecting a ribose derivative and a cytosine derivative to condensation reaction in the absence of a catalyst in an aprotic solvent. CONSTITUTION:(A) A 1-alpha-halogeno-2-deoxyribose derivative expressed by formula I (R<1> and R<2> represent hydroxyl group having protecting group; Y is halogen) and (B) a cytosine derivative expressed by formula II (R<3> represents protecting group of hydroxyl group; X is H, halogen atom or alkyl or alkenyl which may be substituted by the above-mentioned atom) are subjected to condensation reaction to provide a 3',5'-di-substituted-2'-deoxy-beta-cytidine derivative expressed by formula III, which is then subjected to eliminating reaction of the protecting groups to afford the objective derivative expressed by formula IV. Furthermore, the components (A) and (B) are preferably subjected to the condensation reaction in the presence of amines.