2,2{40 -Anhydro-ara-cytidine compounds and process of preparation

Abstract

Abstract wherein X is the conjugate base of a strong acid and R is a radical selected from the group consisting of straight or branched chain aliphatic or alicylic radicals containing from 1 through 20 carbon atoms; monocyclic or bicyclic aromatic radicals of from 6 through 20 carbon atoms; monocyclic heterocyclic radicals of from 4 through 10 carbon atoms; araliphatic radicals of from 7 through 12 carbon atoms; or cage-type hydrocarbon radicals containing from 7 through 20 carbon atoms; and including such radicals substituted by halogen, hydroxyl, carboxyl, nitro, alkoxyl or mercapto substituent groups. It also pertains to the preparation from compounds of formulas I and II of 5''-O-acylates of ara-cytidine. Further, it pertains to pharmaceutical compositions of compounds of formulas I and II and a process for treatment of pathological conditions therewith. Compounds of formulas I and II have immunosuppressive activities. and the acid addition salts thereof. It also pertains to the preparation of novel 5''-O-acyl-2,2''-anhydro-ara-cytidines of the formula II This invention relates to a novel process for preparing the known useful compound 2,2''-anhydro-ara-cytidine (also known as O2, 2''-anhydro-ara-cytidine and O2O2 -anhydro-1- Beta -Darabinofuranosylcytosine) having the formula I

Inventors

• 👤 William J Wechter
• 👤 Duane T Gish

Bibliographic Details