Process for preparation of 1.alpha.,25-dihydroxycholecalciferol

C - Chemistry – Metallurgy – 07 – C

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204/91.05, 260/6

C07C 35/21 (2006.01) C07J 9/00 (2006.01) C07J 71/00 (2006.01)

Patent

CA 1069939

ABSTRACT 1.alpha., 25-dihydroxycholecalciferol is prepared by reacting 1,5,7- trien-3.beta.,25-diol with a 1,2,4-triazoline-dione derivative represented by the formula: Image wherein R represents an alkyl group or an aryl or substituted-aryl group; reacting the resulting 1,4-cyclic adduct represented by the general formula Image wherein R is as defined above, with a peroxide to form a 1.alpha.,2.alpha.-epoxide - 1 - compound represented by the general formula Image wherein R is as defined above, reducing the so formed compound with a metal hydride to form cholesta-5,7-diene-1.alpha.,3.beta.,25-triol, irradiating the so formed compound with ultraviolet rays to form 1.alpha.,25-dihydroxy- previtamin D3, isomerizing the so formed previtamin D3, and recovering 1.alpha.,25-dihydroxycholecalciferol.

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