发明授权
US5166330A Process for the preparation of nucleoside alkyl-aralkyl- and aryl-phosphonites and -phosphonates 失效
核苷烷基 - 芳烷基 - 和芳基 - 亚膦酸酯和膦酸酯的制备方法

Process for the preparation of nucleoside alkyl-aralkyl- and
aryl-phosphonites and -phosphonates
摘要:
Deoxyribonucleoside phosphonates, thiophosphonates and selenophosphonates are obtained by condensation of a difunctional phosphonylating reagent of the formulaR--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 presents 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 thiophosphonates and selenophosphonates and the intermediates of the first condensation stage are new.
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