Research, Incorporated

Yung-Chi Cheng

Miroslav V Bobek

Alexander Bloch

David C Ward

John P Neenan

H William Prusoff

Novel arabinofuranosyl nucleosides and nucleotides having 2'-azido,2'-amino, or 2'-hydrocarbylamino substituents, which have antitumor, antiviral, and antimicrobial properties, are prepared by condensation of a pyrimidine, purine, or 1,3-oxazine base with an acylated 2-azido-2-deoxyarabinofuranosyl halide, followed by deblocking and catalytic hydrogenation, where appropriate, to convert the 2'-azido group to a 2'-amino group and, if desired, alkylation or the like to convert the 2'-amino group to a 2'-hydrocarbylamino group.

Process of preparing 2-azido-2-deoxyarabinofuranosyl halides

Novel arabinofuranosyl nucleosides and nucleotides having 2'-azido, 2'-amino, or 2'-hydrocarbylamino substituents, which have antitumor, antiviral, and antimicrobial properties, are prepared by condensation of a pyrimidine, purine, or 1,3-oxazine base with an acylated 2-azido-2-deoxyarabinofuranosyl halide, followed by deblocking and catalytic hydrogenation, where appropriate, to convert the 2'-azido group to a 2'-amino group and, if desired, alkylation or the like to convert the 2'-amino group to a 2'-hydrocarbylamino group.

2-Substituted arabinofuranosyl nucleosides and nucleotides

The compounds 5'-amino-2',5'-dideoxy-5-iodouridine; 5'-amino-2',5'-dideoxy-5-bromouridine; and the pharmaceutically acceptable acid addition salts thereof have been found to be potent inhibitors of herpes simplex virus.

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Buffalo, NY, United States of America

Yung-Chi Cheng