Regioselective synthesis and anti-HIV activity of the novel 2- and 4-substituted pyrazolo[4,5-e] [ 1,2,4]thiadiazines 被引量：1

Regioselective synthesis and anti-HIV activity of the novel 2- and 4-substituted pyrazolo[4,5-e] [ 1,2,4]thiadiazines

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摘要 The new regioisomer 7-methyl-pyrazolo[4,5-e][1,2,4]thiadiazine nucleus (5) was synthesized, and its novel mono-N2- or N4-substituted pyrazolo[4,5-e][1,2,4]thiadiazines (6, 7) were regioselectively prepared by deprotonation of N2 or/and N4 atoms with different molar ratio of NaH and alkyl halides. Anti-HIV-1 screening tests showed some compounds to be potent as HIV-1 non-nucleoside reverse transcriptase inhibitors (HIV-1 NNRTIs).

作者 Xin Yong Liu Ren Zhang Yan Nian Gen Chen Wen Fang Xu

机构地区 [a]Institute of Medicinal Chemistry

出处《Chinese Chemical Letters》 SCIE CAS CSCD 2007年第2期137-140,共4页 中国化学快报（英文版）

关键词 Pyrazolo[4 5-e][1 2 4]thiadiazine Regioselectivity SYNTHESIS HIV-1 NNRTIs Pyrazolo[4,5-e][1,2,4]thiadiazine Regioselectivity Synthesis HIV-1 NNRTIs

分类号 TQ460.1 [化学工程—制药化工] O626 [理学—有机化学]

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参考文献7

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Chinese Chemical Letters

2007年第2期

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Regioselective synthesis and anti-HIV activity of the novel 2- and 4-substituted pyrazolo[4,5-e] [ 1,2,4]thiadiazines 被引量：1

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