PSEUDO-ISOCYTIDINE PROTECTED PSEUDO-ISOCYTIDINE AND METHODS FOR THEIR PREPARATTION

摘要

1477993 Pseudo-isocytidine RESEARCH CORP 20 Jan 1976 [7 Aug 1975]. 02216/76 Heading C2C Pseudo-isocytidine (I) and its acid addition salts are prepared by reacting a 2,3-O-C 1-7 alkylidene-5-O-trityl-D-ribofuranose with a (C 1-7 alkoxycarbonyl methylene) triphenyl phosphorane at elevated temperature to produce a C 1-7 alkyl 2-(2,3-C 1-7 alkylidene-5-O-trityl-D- ribofuranosyl)acetate (II) which is reacted with a C 1-7 alkyl formate in the presence of an alkali metal hydride to produce a C 1-7 alkyl 2-formyl- 2 - (2,3 - O - C 1-7 alkylidene - 5 - O - trityl - D- ribofuranosyl) - acetate alkali metal enolate (III) which is reacted with guanidine or an acid addition salt thereof to form a novel 5-(2,3- O - C 1-7 alkylidine - 5 - O - trityl - D - ribofuranosyl) - isocytosine (IV) which is treated with a C 1-7 alkanol/mineral acid at 15‹ to 25‹ C. Compound III may be reacted with diazo-C 1-7 alkane to form C 1-7 alkyl 2-C 1-7 alkoxy - methylidene - 2 - (2,3 - O - alkylidene - 5- O - trityl - D - ribofuranosyl) - acetate which may be used in the subsequent reaction. Compounds I may be converted to their acid addition salts. Compounds I may be used as cytostatic, anti-leukemic or anti-viral agents.