The kinetic resolution of racemic 2-O-acylated 3-butene-1, 2-diol and 1-O-acylated 3-butene- 1, 2-diol derivatives by enzymatic saponification and enzymatic esterification, respectively, is investigated with several lipases and esterases. The resulting partially blocked enantiomers are glycosylated with glycosyl halides and trichloroacetimidates, respectively.