Preparation of gABA and L-glutamic acid analogs for antiseizure treatment.

Abstract

Title compds. H2N-CHR3-CR1R2-CH2-CO2H [R1 = C1-6 straight or branched alkyl, Ph, C3-6 cycloalkyl; R2 = H, Me; R3 = H, Me, CO2H] are prepd. E.g., (S)-(+)-4-amino-3-(2-methylpropyl)butanoic acid was prepd. in many steps from 4-methylpentanoic acid, methylphenyloxazolinone, benzyl bromoacetate, and tosyl chloride. Intermediates prepd. during the synthesis of the compd. are further disclosed. In an in vivo study (R)-3-methyl-4-aminobutanoic acid at 30 mg/Kg i.v. protected 4 out of 5 mice from electroshock. [on SciFinder(R)]