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Three natural diosgenyl glycosides: Ophipogonin C (A), Polyphillin C (B), diosgenyl α-L-rhamnopyranosyl-(1→4)-β-D-glucopyranoside (DRG) (C) and one of their analogue diosgenyl α-L-rhannopyranosyl-(1→6)-β-D-glucopyranoside (D) were first systemic synthesiz