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 |
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| Authors: | Sakagami Kazunari Kumagai Toshihito Taguchi Takeo Nakazato Atsuro |
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| Affiliation: | Medicinal Research Laboratories, Taisho Pharmaceutical Co., Ltd., Saitama, Japan. kazunari.sakagami@po.rd.taisho.co.jp |
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| Abstract: | 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. |
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