Highly efficient one-pot synthesis of D-ring chloro-substituted neocryptolepines via a condensation—Pd-catalyzed intramolecular direct arylation strategy

D-ring chloro-substituted neocryptolepines have been synthesized in excellent yield starting from 3-bromo-2-chloro-1-methylquinolinium triflate via a one-pot condensation—Pd-catalyzed intramolecular direct arylation strategy involving chloroanilines. The 3-bromo-2-chloro-1-methylquinolinium triflate was obtained via methylation of commercial 3-bromo-2-chloroquinoline with methyl triflate.

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