An Efficient, One-Pot Transamidation of 8-Aminoquinoline Amides Activated by Tertiary-Butyloxycarbonyl

An Efficient, One-Pot Transamidation of 8-Aminoquinoline Amides Activated by Tertiary-Butyloxycarbonyl

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The efficient, one-pot access to the transamidation of 8-aminoquinoline (8-AQ), Gift Card notorious for its harsh removal conditions, has been widely employed as an auxiliary in C–H functionalization reactions due to its strong directing ability.In this study, the facile and mild Boc protection VCPs of the corresponding 8-AQ amide was critical to activate the amide C(acyl)–N bond by twisting its geometry to lower the amidic resonance energy.Both aryl and alkyl amines proceeded transamidation in one-pot, user-friendly conditions with excellent yields.