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Synthesis and anti-retroviral activity of O,O'-bis(3'-azido-2',3'-dideoxythymidin-5'-yl) phosphoramidate derivatives. 1999
I Kers, and
J Stawiński, and
J L Girardet, and
J L Imbach, and
C Périgaud, and
G Gosselin, and
A M Aubertin
Department of Organic Chemistry, Arrhenius Laboratory, Stockholm University, Sweden.
A simple and efficient protocol for the preparation of various symmetrical dinucleoside phosphoramidates derived from AZT, is presented. It consists of the phosphonylation of AZT with phosphonic acid in the presence of DCC to produce the symmetrical H-phosphonate diester, followed by its oxidative conversion to various phosphoramidate analogues. The synthesized compounds were evaluated for their anti-HIV activity in different cell cultures.
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