Substituted morpholine-2S-acetic acid derivatives: SCH 50911 and related compounds as novel GABA(B) antagonists

Article abstract of DOI:10.1016/S0960-894X(96)00267-3

The synthesis and GABA(B) antagonist activity of a series of substituted morpholine-2-acetic acid derivatives is described. Resolution of the lead compound from the series produces one active and one inactive enantiomer. X- ray analysis of a halogenated derivative (25) of the active enantiomer Sch 50911 (23) shows that it possesses the 2S configuration.