Regioselective and Guided C–H Activation of 4‑Nitropyrazoles

A divergent and regioselective approach
to 5-aryl-4-nitro-1H-pyrazoles was developed by guided
transition-metal-catalyzed
arylation of 4-nitro-1H-pyrazoles. This method provides
a convenient tool for the functionalization of the pharmacologically
relevant pyrazole scaffold. The scope and limitations of the methodology
were studied.

本研究通过导向过渡金属催化（transition-metal-catalyzed）的4-硝基-1H-吡唑（4-nitro-1H-pyrazoles）芳基化反应，开发了一种制备5-芳基-4-硝基-1H-吡唑（5-aryl-4-nitro-1H-pyrazoles）的区域选择性发散合成策略。该方法可为药理相关吡唑骨架的官能化修饰提供便捷合成手段。本研究对该合成方法的适用范围与局限性进行了系统探究。