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A series of novel thiazole-containing triazole antifungals was synthesized and evaluated for antifungal activity against a variety of clinically isolated pathogenic fungi in vitro and against systemic candidosis in vivo. These compounds showed potent antifungal activities in vitro and in vivo. In particular, (2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4- difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (12g; ER-30346) showed potent and well-balanced in vitro activities and potent in vivo efficacy, and had a good safety profile.

Catalytic and stereoselective glycosylation with glycosyl fluoride using carbocationic species paired with tetrakis(pentafluorophenyl)borate [B(C6F5)4−] or trifluoromethanesulfonate (TfO−) is investigated. When the glycosylation is carried out using the former catalyst in dichloromethane containing tBuCN, the major product is β-glycoside while α-selectivity is observed when the latter catalyst in dichloromethane containing Et2O is used. In addition to the characteristic properties of the solvent, the nature of the counter anion such as B(C6F5)4− or TfO− plays important roles in controlling the selectivity. Thus, an appropriate combination of catalyst and solvent leads to the formation of disaccharides.

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