Zhuang Shi-Yi, Tang Yong-Xing, Liu Jin-Yi, Chen Xiang-Long, Ma Jin-Tian, Wu Yan-Dong, Zheng Kai-Lu, Wu An-Xin
Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, P.R. China.
Guangdong Provincial Key Laboratory of Research and Development of Natural Drugs, School of Pharmacy, Guangdong Medical University, Dongguan 523808, P.R. China.
Org Lett. 2022 Apr 22;24(15):2858-2862. doi: 10.1021/acs.orglett.2c00813. Epub 2022 Apr 8.
An I-DMSO-mediated cascade reaction using methyl ketones and 1,2,3,4-tetrahydroisoquinolines (THIQs) as commercially available substrates has been developed for the construction of pyrrolo[2,1-]isoquinoline derivatives. This metal-free process involves N-H/α-C(sp)-H difunctionalization of THIQ. Two C-C bonds and one C-N bond are formed in one pot under mild conditions. Besides, a quaternary carbon center has been constructed in this transformation efficiently.
已开发出一种由二甲亚砜介导的级联反应，该反应使用甲基酮和1,2,3,4-四氢异喹啉（THIQs）作为市售底物来构建吡咯并[2,1 -]异喹啉衍生物。这种无金属过程涉及THIQ的N - H/α - C(sp³)-H双官能团化。在温和条件下，一锅法形成了两个C - C键和一个C - N键。此外，在该转化过程中高效构建了一个季碳中心。
