An overview on lipase-catalyzed enantioselective acylations of diols i
n organic solvents is presented. The application of this biocatalytic
process on diols as a special type of bifunctional compounds as substr
ates is directed on the synthesis of enantiomerically pure building bl
ocks. Prochiral acyclic and cyclic diols can be successfully made asym
metric by using different types of lipases and acylating agents. The k
inetic resolution of racemic cyclic and acyclic diols is demonstrated
by various examples.