Benzoheterocyclylalkylaminoalkanediphosphonic acids

Details Benzoheterocyclylalkylaminoalkanediphosphonic acids Benzoheterocyclylalkylaminoalkanediphosphonic acids

C - Chemistry, Metallurgy

07

F

C07F 9/655 (2006.01) A61K 31/66 (2006.01) C07F 9/6553 (2006.01)

Patent

CA 2053599

4-18407/A Novel benzoheterocyclylalkylaminoalkanediphosphonic acids Abstract of the Disclosure Benzoheterocyclylalkylaminoalkanediphosphonic acids of formula I Image (I) wherein R1 and R2, independently of one another, are hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, R3 is hydrogen or lower alkyl, X and Y, independently of one another, are oxy or thio, alkl and alk2 are identical or different lower alkylene radicals, n is 0 or 1 and m and m', independently of one another, are 0, 1 or 2, the sum of n, m and m' being 1, 2 or 3, and their salts exhibit a pronounced regulatory action on the calcium metabolism of warm-blooded animals. They are prepared, for example, as follows: in a compound of the formula Image (II) wherein R1, R2, n, m, m', X, Y, alk1 and alk2 are as defined above, R'3 is one of the groups R3 mentioned above or is an amino-protecting group R0, Z1 is a functionally modified phosphono group and Z2 is a free or functionally modified phosphono group, converting functionally modified phosphono Z1 and, where appropriate, Z2 into the free phosphono group, and, if desired, converting a resulting compound into a different compound of formula I, separating a mixture of isomers obtainable in accordance with the process into the components and separating the preferred isomer, and/or converting a free compound obtainable in accordance with the process into a salt or converting a salt obtainable in accordance with the process into the corresponding free compound.

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