Enantioselective deacetylation of a-(±)-botryodiplodin acetate was successfully accomplished by means of lipase PS to afford (+)-botryodiplodin and a-(+)-botryodiplodin acetate with high enantiomeric excesses. Enzyme-mediated transesterification of the acetylated molecule with n-butanol, as well as its hydrolysis in several organic solvents, are also reported. The CD spectra of (+)-botryodiplodin and a-(+)-botryodiplodin acetate are also presented.