Abstract

This contribution reports for the first time the late-stage C–H activation of pyrazolo[3,4-b]pyridine derivatives. A family of 16 molecules functionalized on the C-3 position by this methodology is demonstrated. After a careful optimization, a reliable procedure has been developed with Pd(phen)₂(PF₆)₂ catalyst (10 mol%), affording C-3 arylated pyrazolo[3,4-b]pyridines in yields ranging from 40 to 81%.

This contribution reports for the first time the late-stage C–H activation of pyrazolo[3,4-b]pyridine derivatives. A family of 16 molecules functionalized on the C-3 position by this methodology is demonstrated. After a careful optimization, a reliable procedure has been developed with Pd(phen)₂(PF₆)₂ catalyst (10 mol%), affording C-3 arylated pyrazolo[3,4-b]pyridines in yields ranging from 40 to 81%.

中文翻译：

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吡唑并[3,4-b]吡啶的区域选择性晚期C-3功能化

摘要

该贡献首次报道了吡唑并[3,4- b ]吡啶衍生物的后期C–H活化。证明了通过这种方法在C-3位置功能化的16个分子家族。经过仔细的优化后，已经开发出了一种可靠的程序，使用Pd（phen）₂（PF ₆）₂催化剂（10 mol％），可提供C-3芳基吡唑并[3,4- b ]吡啶，产率为40-81 ％。

该贡献首次报道了吡唑并[3,4- b ]吡啶衍生物的后期C–H活化。证明了通过这种方法在C-3位置功能化的16个分子家族。经过仔细的优化后，已经开发出了一种可靠的程序，使用Pd（phen）₂（PF ₆）₂催化剂（10 mol％），可提供C-3芳基吡唑并[3,4- b ]吡啶，产率为40-81 ％。