The synthesis and GABA(B) antagonist activity of a series of substitut
ed morpholine-2-acetic acid derivatives is described. Resolution of th
e lead compound from the series produces one active and one inactive e
nantiomer. X-ray analysis of a halogenated derivative (25) of the acti
ve enantiomer Sch 50911 (23) shows that it possesses the 2S configurat
ion. Copyright (C) 1996 Elsevier Science Ltd