I2-DMSO Mediated Multicomponent [3+2] Annulation Reaction: An Approach to Pyrrolo[2,1-a]isoquinoline Derivatives with a Quaternary Center

作者：Zhuang, Shi-Yi; Liu, Jin-Yi; Guo, Hui; Tang, Yong-Xing; Chen, Xiang-Long; Ma, Jin-Tian; Wu, Yan-Dong; Wu, An-Xin^*; Zheng, Kai-Lu^*

来源：Organic Letters, 2022, 24(46): 8573-8577.

DOI：10.1021/acs.orglett.2c03651

• CYCLOPROPENONES
• CYCLOADDITION
• HETEROCYCLES
• ACTIVATION
• ACCESS

An I2-DMSO mediated multicomponent [3+2] cascade annulation reaction using methyl ketones, 1,2,3,4tetrahydroisoquinolines (THIQ) and cyclopropenones as readily available substrates has been developed. This metal-free process involves N-H/alpha-C(sp3)-H trifunctionalization of THIQ and C- C bond cleavage of cyclopropenone, providing a direct approach to obtain pyrrolo[2,1-a]isoquinoline derivatives with a quaternary carbon center. Two C-C bonds and one C-N bond are formed efficiently in one pot.

• 单位
  广东医学院