Using a chemoselective, sustainable and highly efficient method, new 4-thiazolidinones and 1,4-thiazepan-3-ones substituted with a glycosidic residue derived from D-fructose were synthesized. Microwave-assisted cascade multicomponent reaction under solvent-free conditions gave very good yields in short reaction times, which was followed by a nontoxic purification method of one of the diastereomers by precipitation-centrifugation. The new purified compounds isolated as diastereomers were evaluated as factor Xa (FXa) inhibitors.