M. Begtrup et Fa. Slok, EQUILIBRIUM CONTROL IN BROMOMETHYLATION - AN EXPEDIENT ROUTE TO AMINO-3-(3-HYDROXY-5-METHYLISOXAZOL-4-YL)PROPIONIC ACID (AMPA), Synthesis, (9), 1993, pp. 861-863
The excitatory amino acid amino-3-(3-hydroxy-5-methylisoxazol-4-yl)pro
pionic acid (AMPA) has been prepared in gram quantities in 42 % total
yield by a three-step procedure from 3-hydroxy-5-methylisoxazole. It i
s shown how bromomethylation may be optimized through control of the i
nvolved equilibria and how N-protecting methoxymethyl groups can be re
moved.