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The first arylation strategy for the synthesis of enantioenriched propargylamines is disclosed. This approach, which is complementary to previous alkynylation and alkylation strategies, involves a C(sp2)−C(sp3) bond formation, and is based on the first asymmetric Friedel–Crafts‐type arylation reaction of C‐alkynyl imines. Asymmetric Friedel–Crafts reactions with electron‐deficient phenols, a longstanding...
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