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ChemInform Abstract: Enantioselective Synthesis of (S)-2-Amino-3-(3-Hydroxy-5- methylisoxazol-4-yl)propanoic Acid (S)-AMPA.

โœ Scribed by R. AMICI; P. PEVARELLO; M. COLOMBO; M. VARASI

Publisher
John Wiley and Sons
Year
2010
Weight
30 KB
Volume
28
Category
Article
ISSN
0931-7597

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We have previously shown that whereas (RS)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid (APPA) shows the characteristics of a partial agonist at (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) receptors, (S)-APPA is a full AMPA receptor agonist and (R)-APPA a weak

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RS)-2-Amino-2-(3-hydroxy-5-methylisoxazol-4-yl)acetic acid (AMAA) is a potent and selective agonist at the NMDA subgroup of excitatory amino acid receptors. To probe its interaction with these receptors we have developed a synthesis of [3H]AMAA. Bromination of a protected form of AMAA with NBS follo