Ouyang Jia-Sheng, Zhang Xinhuan, Pan Bendu, Zou Haobin, Chan Albert S C, Qiu Liqin
School of Chemistry, IGCME, Guangdong Key Lab of Chiral Molecules and Drug Discovery, Sun Yat-sen University, Panyu, Guangzhou 510006, China.
School of Pharmacy, Youjiang Medical University for Nationalities, Baise 533000, China.
Org Lett. 2023 Oct 20;25(41):7491-7496. doi: 10.1021/acs.orglett.3c02651. Epub 2023 Oct 10.
Using the robust -heterocyclic carbene-palladium complex (SIPr)Pd(cin)Cl, a highly efficient and easy-to-operate method has been developed at room temperature for the solvent-free Buchwald-Hartwig amination of heteroaryl chlorides with various amines. The amount of catalyst can be as low as 0.05 wt %. The system was demonstrated on 47 substrates and successfully applied to the synthesis of commercial pharmaceuticals and candidate drugs with high yields. Furthermore, the protocol can be used to prepare aniline derivatives on a multigram scale without yield loss.
使用强碱性杂环卡宾-钯配合物（SIPr）Pd（cin）Cl，已开发出一种高效且易于操作的方法，可在室温下实现杂芳基氯化物与各种胺的无溶剂布赫瓦尔德-哈特维希胺化反应。催化剂用量可低至0.05 wt%。该体系在47种底物上得到验证，并成功应用于高产率合成商业药物和候选药物。此外，该方法可用于制备克级规模的苯胺衍生物且不损失产率。
