Fluorine derivatives of vitamin d _and process for producing...

C - Chemistry – Metallurgy – 07 – C

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167/147, 260/581

C07C 401/00 (2006.01) A61K 31/59 (2006.01) C07J 9/00 (2006.01) C07J 71/00 (2006.01)

Patent

CA 1297869

ABSTRACT OF THE DISLCOSURE There are disclosed novel derivatives of 26,26,26,27,27,27-hexafluorovitamin D3 having fluorine atom at the 23- and/or 24-position which have an excellent pharmacological activity and a process for production thereof. The novel compounds are represented by the general formula: Image wherein R1' denotes a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R2 denotes a hydrogen atom or a protecting group for hydroxyl group, R3 denotes a hydrogen atom, a fluorine atom, a hydroxyl group or a protected hydroxyl group and R4 and R4' each denotes a hydrogen atom, or one of them denotes a hydrogen atom and the other denotes a fluorine atom, hydroxyl group or a protected hydroxyl group or R4 and R4' are combined to denote an oxo group, with a proviso that at least one of R3, R4 and R4' denotes a fluorine atom. The process for production thereof comprises subjecting to thermal isomerization a compound represented by the general formula: Image wherein R1', R2, R3, R4 and R4' are the same as defined above, to thermal isomerization and optionally further to deprotection reaction.

549562

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