Department of Chemistry, National University of Singapore, 3 Science Drive 3, 117543 Singapore.
Department of Medicinal Chemistry, School of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China.
J Org Chem. 2023 Jun 16;88(12):7755-7763. doi: 10.1021/acs.joc.2c01369. Epub 2022 Oct 31.
We present herein a novel cobalt/zinc bimetallic catalysis system for the realization of an efficient and enantioselective alkynylation of isatins and α-ketoesters using terminal alkynes. By using a simple procedure with all commercially available catalysts, including cobalt bromide, a chiral bisphosphine ligand, and zinc triflate, a range of synthetically useful tertiary propargylic alcohols are accessed with high yields and good enantioselectivities. Control reactions showed that this catalytic system proceeds through activation of the terminal alkyne by zinc triflate and a base, transmetalation from zinc to cobalt, and then the enantio-determining alkynylation of ketones.
我们在此展示了一种新型的钴/锌双金属催化体系,用于实现高效和对映选择性的吲哚满酮和α-酮酯的炔基化反应,使用末端炔烃作为原料。通过使用一种简单的方法,使用所有商业可得的催化剂,包括溴化钴、手性双膦配体和三氟甲磺酸锌,可以获得一系列具有高收率和良好对映选择性的合成有用的叔炔丙醇。控制反应表明,该催化体系通过三氟甲磺酸锌和碱对末端炔烃的活化、锌到钴的转金属以及随后的酮的对映选择性炔基化反应来进行。