Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering, Southwest University , Chongqing 400715, P. R. China.
J Org Chem. 2018 Feb 2;83(3):1591-1597. doi: 10.1021/acs.joc.7b02857. Epub 2018 Jan 10.
3-Alkyl/aryl-1H-indazoles and 3-alkyl/aryl-3H-indazole-3-phosphonates were synthesized efficiently through a 1,3-dipolar cycloaddition reaction between α-substituted α-diazomethylphosphonates and arynes under simple reaction conditions. The product distribution was controlled by the phosphoryl group, which acted both as a tuning group and a traceless group in the reaction.
3-烷基/芳基-1H-吲唑和 3-烷基/芳基-3H-吲唑-3-膦酸酯通过α-取代的α-重氮甲基膦酸酯与芳炔之间的 1,3-偶极环加成反应在简单的反应条件下高效合成。产物分布由磷酰基控制，磷酰基在反应中既作为调谐基团又作为无痕迹基团。
