N-6 and 5'-n substituted carboxamidoadenosine derivatives as...

Details N-6 and 5'-n substituted carboxamidoadenosine derivatives as... N-6 and 5'-n substituted carboxamidoadenosine derivatives as...

C - Chemistry, Metallurgy

07

H

167/202, 260/229

C07H 19/167 (2006.01) A61K 31/70 (2006.01) C07H 19/16 (2006.01)

Patent

CA 1285557

N-6 AND 5'-N SUBSTITUTED CARBOXAMIDOADENOSINE DERIVATIVES AS CARDIAC VASODILATORS AND ANTI-HYPERTENSIVE AGENTS, AND PROCESS FOR MAKING SAID COMPOUNDS ABSTRACT OF THE DISCLOSURE Compounds of the formula Image are disclosed, wherein R1 represents secondary alkyl; aralkyl; cycloalkyl; heteroaryl substituted alkyl; norbornyl; and substituted secondary alkyl, aralkyl, cycloalkyl, heteroaryl substituted alkyl, norbornyl; and para-substituted phenyl groups; and R2 and R3 are hydrogen or pharmacologically acceptable acyl groups. The compounds of the invention are useful as cardiovascular vasodilator or anti-hypertensive agents. The therapeutically useful compounds of the invention as well as similar 5'-N and N-6 substituted adenosine 5'-uronamides are prepared, in accordance with a novel process, from isopropylidene (or otherwise suitably blocked) inosine-5'-uronic acid. Isopropylideneinosine-5'-uronic acid is reacted with a suitable inorganic acid halide, such as thionyl chloride, to yield 6-halogeno-9-[2',3'-O-isopropylidene-.beta.-D-ribofuranosyl- 5-uronic acid halide]-9H-purine. This intermediate is reacted with an amine of the general formula R4,R5NH to give a 6-halogeno substituted, substituted uronic acid amide of the formula Image wherein X is halogen. Reaction of the latter intermediate with an amine of the formula R1-NH2, and removal of the isopropylidene (or other) blocking groups yields the compounds of the invention.

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