N6 -substituted adenosines

Claim 1

Process for the preparation of N 6 -substituted adenosines of the general Formula I ##SPC4## wherein R 1 and R 2 being the same or different represent hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 7 to 10 carbon atoms unsubstituted or substituted with hydroxy or alkoxy with 1-4 carbon atoms, monocyclic carboxylic aryl unsubstituted or substituted with hydroxyl or alkoxy with 1 to 4 carbon atoms, a heterocyclic ring of 4 to 7 ring members, containing a total of 1-3 nitrogen atoms, or an oxygen or sulfur atom; or when R 1 is hydrogen R 2 is hydroxyl, amino, alkyl or 1-4 carbon atoms substituted in the terminal position with a mono- or dialkylamino group, containing 1-4 carbon atoms in each alkyl group, or a mono- or bicyclic heterocyclic group of 5-10 members, containing a total of 1-3 hetero atoms, which can be nitrogen, oxygen and sulfur, or R 1 and R 2 , together with the N-atom, collectively represent a heteromonocyclic ring of 4-7 members containing a total of 1-3 hetero atoms which, in addition to the nitrogen atom, can be nitrogen, oxygen or sulfur, unsubstituted or substituted by an alkyl group with 1-4 carbon atoms, R 3 represents hydrogen or amino, and Z represents a ribofuranosyl residue, said process comprising reacting a 6-trialkylsilyloxypurine derivate of the general Formula II ##SPC5## wherein the alkyl residues are the same and each alkyl is of 1 to 3 carbon atoms, R 3 ' represents hydrogen or a trialkylsilylamino group wherein the alkyl is of 1 to 3 atoms, Z' represents a silylated or carboxylic acid acylated sugar residue, or a sugar residue blocked by acetal formation, with a member selected from the group consisting of ammonia, an amine of the formula HNR 1 R 2 , wherein R 1 and R 2 have the above designations, and a salt of said amine, in the presence of a tertiary base.