Developing an efficient route to the synthesis of nucleoside 1-alkynylphosphonates

Abstract

A series of ribonucleoside 1-alkynylphosphonates have been synthesized using a palladium-catalyzed phosphonylation of terminal 1,1-dibromo-1-alkene nucleosidic derivatives and high selectivity for product distribution was observed during this step. Both nucleosidic and osidic pathways were explored and the corresponding optimization study is reported herein. © 2009 Elsevier Ltd. All rights reserved.