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The asymmetric Pictet–Spengler reaction (PSR) with aldehydes is well known. However, PSR involving ketones as electrophilic partners is far‐less developed. We report herein the first examples of catalytic enantioselective PSR of tryptamines with α‐ketoamides. A new class of easily accessible prolyl‐urea organocatalysts bearing a single H‐bond donor function catalyzes the title reaction to afford 1,1‐disubstituted...
The asymmetric Pictet–Spengler reaction (PSR) with aldehydes is well known. However, PSR involving ketones as electrophilic partners is far‐less developed. We report herein the first examples of catalytic enantioselective PSR of tryptamines with α‐ketoamides. A new class of easily accessible prolyl‐urea organocatalysts bearing a single H‐bond donor function catalyzes the title reaction to afford 1,1‐disubstituted...
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