Abstract

An intermolecular Ugi reaction of 2-(1-(aminomethyl)cyclohexyl)acetic acid (gabapentin) with aromatic aldehydes and cyclohexyl isocyanide under mild conditions in ethanol has been developed to produce a novel class of N-cyclohexyl-2-(3-oxo-2-azaspiro[4,5]decan-2-yl)-2-aryl acetamides in good to excellent yields. This represents the first Letter for the intermolecular Ugi three component reactions of gabapentin, aromatic aldehydes, and an isocyanide.

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