abstract |
NEW MATERIAL: Compd. expressed by formula I (wherein B is purine, pyrimidine base; R is H, OH protecting group). n EXAMPLE: α,β-(D)-5'-O-benzoyl-2',3'-dideoxycytidine. n USE: Antiviral drug, antibiotic pharmaceutic, drug for the treatment of acquired immunodeficiency syndrome(AIDS) and the like. n PROCESS: A compd. of a group of L- and D-γ-carboxy-γ-butylolactons expressed by formula II is allowed to react with a reducing agent for carboxyl groups. The obtd. hydroxymethyl group is allowed to react with an OH protecting group reagent to be converted into 5-O-hydroxy protecting group-methyl-β- butylolactons expressed by formula III (wherein R is an OH protecting group). Then the product is allowed to react with a reducing agent for carbonyl groups to be converted into 5-O-hydroxy protecting group-methyl-2,3-dideoxy-D or -L-pentofuranose expressed by formula IV, which is then allowed to react with a carbonylating agent expressed by HX (or TMSX). n COPYRIGHT: (C)1989,JPO |