NEW FLUORIDE ANALOG OF VITAMIN D3 AND CELL DIFFERENTIATI0 N INDUCING AGENT CONTAINING THE ANALOG AS ACTIVE COMPONENT

摘要

PURPOSE:To provide a new fluoride analog of vitamin D3 having excellent pharmacologic action, especially antitumor activity caused by the action to induce the cell differentiation from tumor cell to normal cell. CONSTITUTION:The compound of formula I (R<1> to R<3> are H, chemically inactive OH-protecting group, 2-8C acyl or 1-8C alkyl; (n) is 4-6), e.g. 24- homo-26,26,26,27,27,27-hexafluoro-1alpha,25-dihydroxyvitamin D3. The compound can be produced by irradiating a cholestane-5,7-diene compound of formula II with ultraviolet ray in a proper solvent and inert gas atmosphere and heating the resultant previtamin D3 derivative of formula III at 20-120 deg.C, preferably 50-100 deg.C for 1-5hr to effect desired thermal isomerization reaction. Both the starting compound of formula II and the intermediate compound of formula III in the above reaction step are new compounds.