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
A PROCESS FOR THE PRODUCTION OF A COMPOUND OF THE FORMULA
Claim 2
Dependent Claim
11 words
A PROCESS FOR THE PRODUCTION OF A COMPOUND OF THE FORMULA
Claim 3
Dependent Claim
5 words
MIXING 2-AMINO-B-D-ARABINOFURANO-(1'',2'':4,5)-2-OXAZOLINE OF THE FORMULA
Claim 4
Dependent Claim
5 words
MIXING 2-AMINO-B-D-ARABINOFURANO-(1'',2'':4,5)-2-OXAZOLINE OF THE FORMULA
Claim 5
Dependent Claim
20 words
HEATING A THUS PRODUCED COMPOUND RESULTING FROM STEP (1) WITH CYANOACETYLENE TO YIELD A CORRESPONDING COMPOUND OF FORMULA I, ABOVE.
Claim 6
Dependent Claim
20 words
HEATING A THUS PRODUCED COMPOUND RESULTING FROM STEP (1) WITH CYANOACETYLENE TO YIELD A CORRESPONDING COMPOUND OF FORMULA I, ABOVE.
Claim 7
Dependent Claim
20 words
heating a thus produced compound resulting from step (1) with cyanoacetylene to yield a corresponding compound of Formula I, above.
Claim 8
Dependent Claim
20 words
heating a thus produced compound resulting from step (1) with cyanoacetylene to yield a corresponding compound of Formula I, above.
Claim 9
Dependent Claim
23 words
A process in accordance with claim 1 wherein the strong acid is hydrochloric acid and the compound of Formula I is 2,2''-anhydro-ara-cytidine hydrochloride.