GABA Receptor Agonists. Synthesis of Muscimol Analogues Including (R)- and (S)-5-(1-Aminoethyl)-3-isoxazolol and (RS)-5-Aminomethyl-2-isoxazolin-3-ol.

Abstract

The muscimol analogs 4-methyl-5-(2-aminoethyl)-3-isoxazolol, (RS)-5-(1-methyl-2-aminoethyl)-3-isoxazolol, (RS)-4-methyl-5-(1-aminoethyl)-3-isoxazolol, and (RS)-5-(2-aminopropyl)-3-isoxazolol were prepared. The synthesis of (S)- and (R)-5-(1-aminoethyl)-3-isoxazolol from (S)- and (R)-alanine and the synthesis of (RS)-5-aminomethyl-2-isoxazolin-3-ol hydrochloride from (RS)-3-hydroxy-4-aminobutyric acid are described.