Selective glycosylation of the 3-OH of 5,4′-di-O-acetyl-kaempferol was achieved with glycosyl ortho-alkynylbenzoates as donors under the catalysis of Ph3PAuNTf2, and subsequent glycosylation of the remaining 7-OH with glycosyl trifluoroacetimidates under the catalysis of BF3·OEt2, after global deprotection, afforded the kaempferol 3,7-O-bisglycosides conveniently.

Glycosylation of the acid labile betulin and betulinic acid derivatives was achieved with glycosyl ortho-hexynylbenzoates as donors under the catalysis of PPh3AuNTf2; this enabled the efficient synthesis of lupane-type saponins, as exemplified by the total synthesis of the proposed betulinic acid trisaccharide from Bersama engleriana.

Glycosylation of the acid labile protopanaxadiol derivatives was succeeded with a glycosyl ortho-hexynylbenzoate as donor under the catalysis of PPh3AuNTf2, leading to the subsequent elaboration of ginsenoside Rh2 and chikusetsusaponin-LT8 in a concise manner.