Department of Medicinal Chemistry, Research and Early Development, Respiratory and Immunology, BioPharmaceuticals R&D, AstraZeneca Pepparedsleden 1, 43183 Mölndal, Sweden.
University of Strasbourg, 4 Rue Blaise Pascal, 67081 Strasbourg, France.
Chem Commun (Camb). 2022 Jan 18;58(6):827-830. doi: 10.1039/d1cc06337e.
The use of Pd(OAc) as the catalyst and AgOAc as the oxidant enabled the direct regioselective oxidative C-H/C-H cross-coupling of pyrazolo[1,5-]pyrimidines or pyrazolo[1,5-]pyridines with various five-membered heteroarenes without the need of pre-activation and/or directing groups. Successful coupling partners include thiophenes, benzothiophenes, thiazoles, furans, oxazoles, indoles and imidazo[1,2-]pyridines.
使用 Pd(OAc) 作为催化剂和 AgOAc 作为氧化剂，可以实现无需预活化和/或导向基团的直接区域选择性氧化 C-H/C-H 交叉偶联吡唑并[1,5-a]嘧啶或吡唑并[1,5-a]吡啶与各种五元杂芳烃。成功的偶联伙伴包括噻吩、苯并噻吩、噻唑、呋喃、恶唑、吲哚和咪唑并[1,2-a]吡啶。
