Catalyst-free benzylic C(sp³)-H functionalization of methyl quinolines with tryptanthrins

<p>A simple and efficient method of catalyst free for the sp³ C–H bond activation of methyl aza-arene and nucleophilic addition to tryptanthrins in DMF was developed. Importantly, the more efficient and green isolation strategy of the purification of the products by centrifugation with 90% yields was applied.</p

Amino Acid Salts Catalyzed Asymmetric Aldol Reaction of Tryptanthrin: A Straightforward Synthesis of Phaitanthrin A and Its Derivatives

The first asymmetric synthesis of (<i>S</i>)-Phaitanthrin A and its derivatives via a catalytic aldol reaction of Tryptanthrin and ketones is described, in which the cheap, easily prepared natural amino acid salts exhibited unique catalytic ability; importantly, this methodology tolerates a range of substrates with different substitution patterns. Moreover, the synthetic utility of this strategy was further illustrated by a gram-scale synthesis of Phaitanthrin A