Research, Incorporated

Health Research Inc., Roswell Park Division

Miroslav V Bobek

Yung-Chi Cheng

Alexander Bloch

Ralph J Bernacki

Seung-Ho An

Novel arabinopyranosyl nucleoside derivatives having the heterocyclic moiety and fluorine at the 2' position of the sugar ring (pyranose configuration), which have antitumor, antiviral and antimicrobial properties, are prepared by condensation of a pyrimidine, purine or 1,3-oxazine base with an acylated 2-deoxy-2,2-difluoro-D-arabinopyranoside and/or acylated 2-deoxy-2-bromo-2-fluoro-D-arabinopyranoside.

2-substituted arabinopyranosyl nucleosides and nucleotides

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.

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Williamsville, NY, United States of America

Miroslav V Bobek