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Note | Regular issue | Vol 68, No. 6, 2006, pp.1225-1232
Published online, 2nd May, 2006
DOI: 10.3987/COM-06-10707
Regioselective Synthesis of the Novel N4-Substituted Pyrazolo[4,5-e][1,2,4]thiadiazines as Potent HIV-1 NNRTIs

Xinyong Liu,* Niangen Chen, Renzhang Yan, Wenfang Xu, Maria Teresa Molina, and Salvador Vega

*Institute of Medicinal Chemistry, School of Pharmacy, Shandong University, 250012 Jinan, China

Abstract

A new ring system of 7-methylpyrazolo[4,5-e][1,2,4]thiadiazine (5) was synthesized. Starting from 5 a series of novel mono N4-substituted derivatives (6) were prepared regioselectively and evaluated as potent HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs).