The resolution of the enantiomers of the chemotherapeutic Ornidazole (Tiberal®) 1a was achieved by acetylation of the racemic compound with vinylacetate in the presence of lipase Amano PS (from Pseudomonas cepacia). The halogen analogues 4a–6a and the corresponding 4-nitro-derivatives 1b and 4b–6b were also synthesized and the enantiomers were separated by kinetic enzymatic resolution. The absolute configuration of two ...