An Efficient One-Step Synthesis of Heterobiaryl Pyrazolo[3,4-<i>b</i>]pyridines via Indole Ring Opening

A mild one-step synthetic method to access privileged heterobiaryl pyrazolo[3,4-b]pyridines from indole-3-carboxaldehyde derivatives and a variety of aminopyrazoles has been developed. This novel method constructs heterobiaryls with the wide scope of substrate generality and excellent regioselectivity via indole ring opening.本研究开发了一种温和的一步合成方法，可由吲哚-3-甲醛衍生物与多种氨基吡唑类化合物出发，合成得到具有优势杂联芳基结构的吡唑并[3,4-b]吡啶。该新型方法通过吲哚开环反应，构建出底物普适性广、区域选择性优异的杂联芳基产物。