Cui Hai-Lei, Peng Li-Jie, Zhou Hai-Lin, You Xiao-Lin, Jiang Xiao-Jie
International Academy of Targeted Therapeutics and Innovation, Chongqing University of Arts and Sciences, 319 Honghe Ave., Yongchuan, Chongqing 402160, P.R. China.
Org Biomol Chem. 2017 Jun 21;15(24):5121-5125. doi: 10.1039/c7ob01032j.
We have developed a mild, convenient and efficient synthesis of highly functionalized (Z)-β-enamino ketones from readily available 3,4-dihydroisoquinoline imines and ynones through an aza-Michael/hydrolysis cascade reaction. This method is also suitable for the preparation of (Z)-β-enamino esters using alkynoates as starting materials. Complex fully substituted pyrroles can be constructed from the obtained (Z)-β-enamino ketones. It is an attractive alternative approach for the preparation of highly functionalized enamino ketones, esters and pyrroles.
我们通过氮杂迈克尔/水解串联反应，从容易获得的3,4-二氢异喹啉亚胺和炔酮出发，开发了一种温和、便捷且高效的方法来合成高度官能化的(Z)-β-烯胺酮。该方法也适用于以炔酸酯为起始原料制备(Z)-β-烯胺酯。由所得的(Z)-β-烯胺酮可以构建复杂的全取代吡咯。这是一种制备高度官能化烯胺酮、酯和吡咯的具有吸引力的替代方法。
