Synthesis of some 3',5'-dideoxy-5'-C-phosphonomethyl nucleosides. |
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| Authors: | P Ioannidis B Classon B Samuelsson I Kvarnstr?m |
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| Institution: | Department of Organic Chemistry, Arrhenius Laboratory, Stockholm University, Sweden. |
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| Abstract: | Ammonium 1-(3',5',6'-trideoxy-beta-D-erythro-hexofuranosyl)thymine]-6'- phosphonate (1), ammonium 3',5'-dideoxycytidine-5'-C-methylphosphonate (2) and 3',5'-dideoxyadenosine-5'-C-methyl phosphonic acid (3) have been synthesized and tested for anti-HIV activity. The key steps involved an Arbuzov reaction between triethyl phosphite and 3,5,6-trideoxy-6-iodo-1,2-O-isopropylidene-alpha-D-erythro- hexofuranose (7), followed by condensation with the appropriate nucleoside bases. The substances 1, 2 and 3 have been tested in vitro against HIV. |
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