Solid-phase synthesis of N-alkyl amides

Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing

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564133, 564134, 564135, 564136, 564137, 564139, 436 85, 436 86, C07C23102

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058615326

ABSTRACT:
Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.

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