Ao Yunlin, Ma Haowen, Gan Binghan, Wang Wenjing, Zhang Jiehao, Zhou Wei, Zhang Xiaoqi, Cai Qian
College of Pharmacy, Jinan University, No. 601 Huangpu Avenue West, Guangzhou, 510632, P. R. China.
Org Lett. 2024 Jun 7;26(22):4761-4766. doi: 10.1021/acs.orglett.4c01568. Epub 2024 May 29.
A mild copper-catalyzed asymmetric Kinugasa/Michael addition cascade process is developed. The reaction of α, β-unsaturated ester-tethered propiolamides with nitrones provides an efficient protocol for the construction of functionalized chiral 2,6-diazaspiro[3.4]octane-1,5-dione products in satisfactory yields and with high enantio- and diastereoselectivities.
开发了一种温和的铜催化不对称衣笠/迈克尔加成串联反应过程。α，β-不饱和酯连接的丙炔酰胺与硝酮的反应为构建官能化手性2,6-二氮杂螺[3.4]辛烷-1,5-二酮产物提供了一种有效的方法，产率令人满意，对映选择性和非对映选择性高。
