Process for the preparation of nucleoside alkyl-, aralkyl-...

C - Chemistry – Metallurgy – 07 – H

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260/229.1, 195/1

C07H 21/00 (2006.01) C07F 9/48 (2006.01) C07H 19/04 (2006.01)

Patent

CA 1235079

- 1 - Abstract of the disclosure Deoxyribonucleoside phosphonates, thiophosphonates and selenophosphonates are obtained by condensation of a difunctional phosphonylating reagent of the formula R-PXY, in which R is an inert non-cytotoxic organic radical, X is chlorine or Y and Y is a secondary amino group, with a deoxyribonucleoside of which the 5-hydroxyl group and any exo-amino group present in the base radical are protected, and further condensation with a nucleoside of which the 3-hydroxyl group and any exo-amino group present in the base radical are protected, and then oxidation. The thio- phosphonates and selenophosphonates and the intermediates of the first condensation stage are new.

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