PURPOSE: To obtain a novel vitamin D derivative comprising a fluorinated 1α, 25-dihydroxy-hexahydrovitamin D derivative, capable of being obtained from inexpensive raw materials in a large amount, and effective as a therapeutic medicine for renal failure rhachitis, osteoporosis, etc.
CONSTITUTION: A novel 1α, 3β-protected-25-methoxymethyloxy-26,26,26,27, 27,27- hexafluorovitamin D3 of formula I (R1,R2 are a trialkylsilyl, a tetrahydropyranyl). This compound is obtained by reacting a 1α, 3β- protected-20(S)-(p-toluenesulfonyloxymethyl)-9,-10-secopregna-5(Z),7(E),10(19)- toluene of formula II (Ts is p-toluenesulfonyl) with a 1,1'-bis(trifluoromethyl)-1- methoxymethyloxy-3-arylsulfonylpropane of formula III (Ar is an aromatic group) in the presence of an alkyl lithium amide in an anhydrous ether solvent and subsequently treating the reactional product with a phosphate salt and sodium amalgam.
ANDO KAORI
TAKAYAMA HIROAKI
TAKAYAMA HIROAKI