Design and Synthesis of Fluoro Analogues of Vitamin D

The discovery of a large variety of functions of vitamin D(3) and its metabolites has led to the design and synthesis of a vast amount of vitamin D(3) analogues in order to increase the potency and reduce toxicity. The introduction of highly electronegative fluorine atom(s) into vitamin D(3) skeletons alters their physical and chemical properties. To date, many fluorinated vitamin D(3) analogues have been designed and synthesized. This review summarizes the molecular structures of fluoro-containing vitamin D(3) analogues and their synthetic methodologies.