Synthesis of α-6-sulfoquinovosyl-1,2-O-diacylglycerols is achieved by a versatile chemo-enzymatic stereoselective procedure that involves the use of α-d-glucosidase activity from the Mediterranean mollusc Aplysia fasciata. The synthetic procedure is designed to obtain a wide diversity of regio- and stereo-isomers of these compounds that have gained great interest as antineoplastic agents and potent