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Total Synthesis and Glycosidase Inhibition of Broussonetine I and J2

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posted on 19.02.2016, 00:40 by Hui Zhao, Atsushi Kato, Kasumi Sato, Yue-Mei Jia, Chu-Yi Yu
The first total synthesis of both broussonetine I and J2 together with their enantiomers have been accomplished via the same synthetic route through 18 and 16 steps in excellent overall yields (18% and 19%, respectively), starting from R-glyceraldehyde. Broussonetine I was found to be a potent inhibitor of β-glucosidase (IC50 = 2.9 μM), while ent-broussonetine I and ent-broussonetine J2 were found to be potent inhibitors of α-glucosidase (IC50 = 0.33 and 0.53 μM, respectively).