Abstract

AbstractA short and efficient synthesis of the selective human N‐methyl‐D‐aspartate (NMDA) receptor 2A (NR2A) antagonist NVP‐AAM077 is described. The target was achieved in 8 steps and in 54% overall yield from the commercially available chemical 3‐methylbenzene‐1,2‐diamine. A NaIO4/DMF‐based oxidation of the bromide to corresponding aldehyde and an addition of phosphinic acid ester to the aldimine successfully served as the key steps.

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