Routes to 4-substituted analogues of the glycine/NMDA antagonist HA-996. Enantioselective synthesis of (3R,4R) 3-amino-1-hydroxy-4-methyl-2-pyrrolidinone (L-687, 414).

Add time:07/12/2019    Source:sciencedirect.com

Glycine anion (4) and glycine cation (8) synthons are used in efficient syntheses of 4-substituted analogues of HA-966 (1). A stereospecific route to cis derivatives involves hydrogenation of enamines such as 16. Introduction of a chiral auxiliary leads to an enantioselective synthesis of 2a (L-687, 414).

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