| abstract |
Novel 2''-0-, 3''-0-, 2'',3''-di-0-, 2'',5''-di-0- and 3'',5''-di-0esters of ara-cytidine and novel processes for their preparation are claimed. The novel 2''-0-esters (1) and 2'',5''-di-0-esters (11) are embraced by the formula WHEREIN Y is selected from the group consisting of 1. wherein R is a radical selected from the group consisting of aliphatic of from 1 through 20 carbon atoms, aromatic of from 6 through 10 carbon atoms, cage-type hydrocarbon of from 7 through 20 carbon atoms, monocyclic aliphatic of from 4 through 10 carbon atoms, araliphatic of from 7 through 12 carbon atoms and monocyclic heterocyclic of from 4 through 10 carbon atoms, including such radicals substituted by halogen, hydroxyl, carboxyl, nitro, alkoxyl or mercapto groups; 2. wherein R'' is a radical selected from the group consisting of aliphatic of from 1 through 20 carbon atoms, aromatic of from 6 through 10 carbon atoms, araliphatic of from 7 through 12 carbon atoms, AND Z is selected from the group consisting of Y and hydrogen; and pharmaceutically acceptable acid addition salts thereof. The novel 3''-0-esters (III) and 3'',5''-di-0-esters (IV) are embraced by the formula WHEREIN Z and Y are as given above, and pharmaceutically acceptable acid addition salts thereof. The novel 2'',3''-di-0-esters (V) are embraced by the formula WHEREIN Y is as given above, and pharmaceutically acceptable acid addition salts thereof. The compounds of the above formulae are orally active sustainedrelease immunosuppressant and anti-neoplastic agents having the characteristics of the anti-leukemic compound ara-cytidine. |