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2,6-Di(arylamino)-3-fluoropyridine Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors. 2016
Sergey Sergeyev, and
Ashok Kumar Yadav, and
Philippe Franck, and
Johan Michiels, and
Paul Lewi, and
Jan Heeres, and
Guido Vanham, and
Kevin K Ariën, and
Christophe M L Vande Velde, and
Hans De Winter, and
Bert U W Maes
Organic Synthesis Division, Department of Chemistry, University of Antwerp , Groenenborgerlaan 171, B-2020 Antwerp, Belgium.
New non-nucleoside reverse transcriptase inhibitors (NNRTI), which are similar in structure to earlier described di(arylamino)pyrimidines but featuring a 2,6-di(arylamino)-3-fluoropyridine, 2,4-di(arylamino)-5-fluoropyrimidine, or 1,3-di(arylamino)-4-fluorobenzene moiety instead of a 2,4-disubstituted pyrimidine moiety, are reported. The short and practical synthesis of novel NNRTI relies on two sequential Pd-catalyzed aminations as the key steps. It is demonstrated through direct comparison with reference compounds that the presence of a fluorine atom increases the in vitro anti-HIV activity, both against the wild type virus and drug-resistant mutant strains.
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