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An Efficient Synthesis of Selective Human NR2A Antagonist NVP‐AAM077
Author(s) -
Li GangQin,
Su WeiKe,
Yao ZhuJun
Publication year - 2006
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.200690333
Subject(s) - chemistry , yield (engineering) , antagonist , aldimine , bromide , diamine , nmda receptor , aldehyde , receptor antagonist , combinatorial chemistry , stereochemistry , medicinal chemistry , receptor , organic chemistry , biochemistry , materials science , metallurgy , catalysis
A 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 NaIO 4 /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.