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We successfully synthesized the potent and selective group II mGluR agonist (+)-1 (MGS0008) via a process incorporating the key step of efficient fluorination of epoxide (+/-)-5c. This method would be adaptable to large-scale synthesis to produce (+)-1 in multi-gram quantities.

chemical and pharmaceutical bulletin/chemical and pharmaceutical bulletin

Scalable Synthesis of (+)-2-Amino-3-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic Acid as a Potent and Selective Group II Metabotropic Glutamate Receptor Agonist