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Regioselective Synthesis of the Novel N4-Substituted Pyrazolo[4,5-e][1,2,4]thiadiazines as Potent HIV1 NNRTIs

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  2006 Thiadiazine derivativesR 0660 Regioselective Synthesis of the Novel N 4 -Substituted Pyrazolo[4,5-e][1,2,4]thia-diazines as Potent HIV-1 NNRTIs.  — Starting from the pyrazole derivatives (I), the novel thiadiazine regioisomer (IV) is prepared and selectively alkylated at N 4 . The resulting derivatives are evaluated as potential HIV-1 non-nucleoside reverse tran-scriptase inhibitors. Positive results are only observed for (VIb) and the corresponding chloro analogue. — (LIU*, X.; CHEN, N.; YAN, R.; XU, W.; MOLINA, M. T.; VEGA, S.; Heterocycles 68 (2006) 6, 1225-1232; Inst. Med. Chem., Sch. Pharm., Shandong Univ., Jinan 250012, Peop. Rep. China; Eng.) — Mais   42-164
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