A new direct synthesis of ACPA and novel AMPA analogues

A novel synthesis of the potent glutamate neuro transmitter agonist (RS)-2- amino-3-(3-carboxy-5-methyl-4-isoxazolyl) propionic acid (ACPA) provides ac cess to numerous analogues as drug candidates for neurological disorders. T he one-pot synthesis of an alpha amino phosphonate from aldehyde 4 was succ essful using ErCl3 as a catalyst. Molecular modeling of the new amino phosp honic acid with the (RS)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl) propio nic acid (AMPA) receptor crystal structure suggests this should be an effec tive receptor binder. (C) 2001 Elsevier Science Ltd. All rights reserved.