2-Substituted arabinofuranosyl nucleosides and nucleotides

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

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536 23, 536 24, 536 27, 536 28, 536 29, A61K 3170, C07H 1700, C07H 1512, C07H 1700

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042306981

ABSTRACT:
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.

REFERENCES:
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patent: 3809689 (1974-05-01), Damadaran et al.
patent: 3987030 (1976-10-01), Suzuki et al.
Reist, E., et al. J. Organic Chemistry, vol. 32, 2538-2541 (1967).
Unger et al., Tetrahedron Letters, No. 50, pp. 4383-4384 (1977).

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