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• W2320211302 abstract "The organocatalytic site-selective monoacylation of avermectin B2a, an insecticidal and anti-parasitic drug, was accomplished. Although an acetylation of avermectin B2a using a 4-dimethylaminopyridine (DMAP) as a catalyst gave poor site-selectivity, use of our organocatalyst increased site-selectivity of the acylation at the C-5-OH as well as the yield of monoacetate. This catalyst was also effective in other acylations. Interestingly, trihaloacetylation under same conditions gave poor site-selectivity. However, the use of an enantiomer of our organocatalyst provided the C-4″-O-trihaloacetyl avermectin B2a with excellent site-selectivity. These results indicate that the site-selective acylation of avermectin B2a can be controlled by the combination of a suitable organocatalyst and an acid anhydride." @default.
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• W2320211302 date "2016-01-01" @default.
• W2320211302 modified "2023-10-18" @default.
• W2320211302 title "Organocatalytic Site-Selective Acylation of Avermectin B_2a, a Unique Endectocidal Drug" @default.
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• W2320211302 doi "https://doi.org/10.1248/cpb.c16-00205" @default.
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