Synthesis of ertugliflozin from d-glucose |
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| Authors: | Virginia V. Triantakonstanti Thanos Andreou Theoharis V. Koftis John K. Gallos |
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| Affiliation: | 1. Department of Chemistry, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece;2. Pharmathen Industrial S.A., 9th km Thermi-Thessaloniki, Thessaloniki 57001, Greece |
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| Abstract: | A new synthesis of ertugliflozin from d-glucose in 7% overall yield is reported. The reaction sequence involves conversion of d-glucose to a fully protected open chain d-glucose aldehyde in 4 steps, further installation of the aglycon group by a Grignard reaction, introduction of the hydroxymethyl group by a sequential oxidation/aldol reaction/Canizzarro reduction, and finally benzylic oxidation and global deprotection. |
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| Keywords: | Ertugliflozin Grignard reaction Benzylic oxidation SGLT2 inhibitors |
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