Photomediated One-Pot Multicomponent Cascade Reaction for the Synthesis of N-Acyl/Sulfonyl-α-Phosphonated-1,2,3,4-Tetrahydroisoquinoline via Twice Acyl/Sulfonyl Iminium Formation.

N-acyl/sulfonyl-α-phosphonated 1,2,3,4-tetrahydroiso-quinolines (THIQs) are highly important structural motifs in organic synthesis and drug discovery. However, the one-pot approach enabling direct difunctionalization of THIQs remains challenging. Herein we report a photomediated one-pot multicomponent cascade reaction to access N-acyl/sulfonyl-α-phosphonated THIQs via twice acyl/sulfonyl iminium.

Photomediated One-Pot Three-Component Approach Enables the Formal Direct -Acylation/Sulfonylation and α-C-H Functionalization of 1,2,3,4-Tetrahydroisoquinoline.

-Acyl/sulfonyl-α-functionalized 1,2,3,4-tetrahydroisoquinolines (THIQs) are significant structural motifs in organic synthesis and drug discovery. However, the one-pot approach enabling direct difunctionalization of THIQs remains challenging. Herein we report a photomediated one-pot three-component strategy to access -acyl/sulfonyl-α-functionalized THIQs.