Synthesis of glutamate agonists and antagonists by a ring switching strategy

Article abstract of DOI:10.1016/0040-4039(95)01517-5

Our ring switching strategy for synthesis of compounds with structural features consistent with activity at glutamate receptors has been modified to prepare L-alanine derivatives substituted at the β-carbon atom with six-membered heteroaromatic rings. The pyrimidinone (11, R = R¹ = R² = H) has been shown to be a glutamate agonist and the compound (13) to be an antagonist.