Vitamin D is essential for the absorption and utilization of calcium and phosphate and aids in the mobilization of bone calcium and maintenance of serum calcium concentrations. 25-Hydroxyvitamin D₃ is the major circulating metabolite of vitamin D₃.¹

It is produced in the liver and is the best indicator of the body's vitamin D stores. It is effective in the treatment of Rickets and Osteomalacia, both in azotemic and non-azotemic patients. Calcifediol also has mineralizing properties and it is used in clinical situations.

We described herein synthesis of calcifediol from vitamin D₂ based on the Barton-Hesse and their collaborators^2,3 strategy with some modifications of this pathway. Our synthesis of calcifediol can be suitable for the large scale preparation of this important vitamin D analogue.

¹ Deluca, H.F.; Paaren,H.F.; Schnoes, H.K. Top. Curr. Chem. 1979, 83, and references there citted.

² Andrews, D.R.; Barton, D.H.R.; HesseR.H.; Pechet, M.M. J. Org. Chem. 1986, 51, 4819.

³Manchand, P.S.; Yiannikouros, G.P.; Belica, P.S.; Madan, P. J. Org. Chem. 1995, 60, 6574.

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