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Title: Solution-phase parallel synthesis of S-DABO analogues
Authors: Togninelli, Andrea
Carmi, C
Petricci, Elena 
Mugnaini, Claudia 
Massa, Silvio
Corelli, Federico 
Botta, Maurizio 
Issue Date: 2006
Project: None 
A simple and straightforward methodology for the parallel, solution-phase synthesis of a new series of S-DABO derivatives 1 and 2, bearing aromatic substituents at the C2 and C6 positions, has been developed. Starting from potassium ethyl malonates 3, thiouracil intermediates 5 were prepared through parallel synthesis and isolated as pure products by simple extraction with ethyl acetate. Selective S-benzylation of 5 was achieved in few minutes under microwave irradiation to give the title compounds 1, which were oxidized in parallel to the corresponding sulfones 2. Some of the new compounds 1 showed potent inhibitory activity against HIV-1 RT.
ISSN: 0040-4039
DOI: 10.1016/j.tetlet.2005.10.142
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