| 摘要 |
<p>PURPOSE:To provide a new compound useful as a bone absorption inhibitor and a medicine for improving bone diseases. CONSTITUTION:The compound of formula I or II [R is H or a lower alkyl; Y and Z are a (lower alkyl-substituted) 2 to 5C alkylene; X is a single bond or a (lower alkyl-substituted) 1 to 10C alkylene; A-O is a residue of a compound exhibiting an estrogenic activity; q is 1 to 3], its pharmaceutically permissible salt, e.g. (1-piperazinyl)methylenebisphosphonic acid disodium salt. The compound of formula I can be obtained, e.g. by reacting a compound of formula III (Q is an amino-protecting group) with a mixture of triethyl orthoformate and a dialkyl phosphite, catalytically reducing the resultant compound of formula IV in the presence of palladium-carbon in a solvent such as ethanol for eliminating the amino-protecting group from the compound of formula IV and, as necessary, carrying out a further hydrolysis in the presence of a halosilane compound, etc., for eliminating the hydroxyl-protecting group.</p> |
