Abstract
An I2-DMSO mediated multicomponent [3+2] cascade annulation reaction using methyl ketones, 1,2,3,4-tetrahydroisoquinolines (THIQ) and cyclopropenones as readily available substrates has been developed. This metal-free process involves N-H/α-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.
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