College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215123, China.
Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Org Biomol Chem. 2020 Mar 14;18(10):1926-1932. doi: 10.1039/d0ob00222d. Epub 2020 Feb 26.
A copper-catalyzed formal [1 + 2 + 2]-annulation of alkyne-tethered diazo compounds with pyridines, which affords polycyclic fused indolizines in synthetically useful to good yields under mild reaction conditions, has been reported. This method features the use of an inexpensive copper catalyst and readily available starting materials, broad substrate generality, and operational simplicity. Notably, a variety of natural product derivatives are compatible under the current conditions, which shows significant potential of this method for the selective decoration and modification of analogous biomolecules or pharmaceuticals.
报道了一种铜催化的炔烃键合重氮化合物与吡啶的[1 + 2 + 2]-环加成的方法，该方法在温和的反应条件下以较高的收率得到了多环稠合的吲唑啉类化合物。该方法的特点是使用了廉价的铜催化剂和易得的起始原料，具有广泛的底物通用性和操作简单性。值得注意的是，在目前的条件下，各种天然产物衍生物都具有兼容性，这表明该方法在选择性修饰和改造类似生物分子或药物方面具有很大的潜力。
