Synthesis of Tofogliflozin as an SGLT2 Inhibitor via Construction of Dihydroisobenzofuran by Intramolecular [4 + 2] Cycloaddition

The synthesis of tofogliflozin (1), a sodium glucose cotransporter 2 (SGLT2) inhibitor, was achieved through the key steps of intramolecular [4 + 2] cycloaddition of dienone-yne intermediate, aerobic aromatization, and anomeric equilibration, thus enabling the construction of a dihydroisobenzofuran...

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Veröffentlicht in:Organic process research & development 2019-04, Vol.23 (4), p.548-557
Hauptverfasser: Murakata, Masatoshi, Kawase, Akira, Kimura, Nobuaki, Ikeda, Takuma, Nagase, Masahiro, Koizumi, Masatoshi, Kuwata, Kazuaki, Maeda, Kenji, Shimizu, Hitoshi
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Sprache:eng
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