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Synthesis of 4-Azaindolines Using Phase-Transfer Catalysis via an Intramolecular Mannich Reaction
journal contribution
posted on 2020-03-11, 14:03 authored by Jingdong Wang, Yuxin Liu, Zhonglin Wei, Jungang Cao, Dapeng Liang, Yingjie Lin, Haifeng DuanA series of bifunctional asymmetric phase-transfer catalysts containing
novel fluorine-containing urea groups derived from cinchona alkaloids
have been synthesized and successfully applied in the asymmetric intramolecular
Mannich reaction. The 4-azaindoline products bearing multiple substrates
were obtained in excellent yield (90−99%), with high enantioselectivity
(up to 95%) and diastereoselectivity (up to >99:1).