The structure-activity relationship of sixteen 3-deaza, C-4 substitute
d pyrimidines and imidazo[1,2-c]pyrimidine bases of 1,3-oxathiolanes a
nd 1,3-dioxolanes revealed good anti-HBV activity in 2.2.15 cells tran
sfected with human hepatitis B virus of the imidazo[1,2-c]pyrimidine n
ucleosides 21, 25 and 29. Two procedures for the preparation of C-4 su
bstituted analogues are reported based on nucleophilic displacement of
a sulfonamide or imidazole by a variety of nitrogen nucleophiles.