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A direct, one-pot sequential reductive bisalkylation method enables the efficient conversion of lactams and amides using Grignard and organolithium reagents via lactam/amide activation. Novelty: ClaimNovelty.METHODOLOGICAL. Consensus alignment: ConsensusAlignment.NEUTRAL.

March 20, 2010Angewandte Chemie International Edition276 citations

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Direct, One‐pot Sequential Reductive Alkylation of Lactams/Amides with Grignard and Organolithium Reagents through Lactam/Amide Activation

KXKai‐Jiong Xiao JLJie‐Min Luo KYKe‐Yin Ye

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Abstract

Be dazzled by the sequence: The first efficient and general one-pot method for the reductive bisalkylation of lactams/amides with Grignard and organolithium reagents has been developed (see scheme; DTBMP=2,6-di-tert-butyl-4-methylpyridine, Tf=trifluoromethanesulfonyl).

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Direct, One‐pot Sequential Reductive Alkylation of Lactams/Amides with Grignard and Organolithium Reagents through Lactam/Amide Activation

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