Liu Duan-Yang, Liu Xu, Gao Yan, Wang Chao-Qun, Tian Jie-Sheng, Loh Teck-Peng
Institute of Advanced Synthesis (IAS), Nanjing Tech University (NanjingTech), Nanjing 211816, P. R. China.
Institute of Advanced Synthesis (IAS), Northwestern Polytechnical University (NPU), Xi'an 710072, China.
Org Lett. 2020 Nov 20;22(22):8978-8983. doi: 10.1021/acs.orglett.0c03382. Epub 2020 Nov 11.
This paper reports a highly site-selective alkylation of heteroarene -oxides using hypervalent iodine(III) carboxylates to serve as an alkylating agent in the presence of a cheap copper catalyst under visible light conditions. This mild method proceeds at room temperature in an air atmosphere and can withstand various heteroarene -oxides as well as various primary, secondary, and tertiary alkyl carboxylic acids. It also provides a practical method for enabling the rapid conversion of commercially available raw materials into medically relevant "drug-like" molecules.
本文报道了一种高度位点选择性的杂芳烃氧化物烷基化反应,该反应使用高价碘(III)羧酸盐作为烷基化剂,在廉价铜催化剂存在下于可见光条件下进行。这种温和的方法在室温空气氛围中进行,能够耐受各种杂芳烃氧化物以及各种伯、仲和叔烷基羧酸。它还提供了一种实用方法,可将市售原料快速转化为与医学相关的“类药物”分子。