【药物名称】Minodronic acid, Ono-5920, YH-529, YM-529, Onobis
化学结构式(Chemical Structure):
参考文献No.12090
标题:Heterocyclic biphosphonic acid derivs.
作者:Isomura, Y.; Takeuchi, M.; Abe, T. (Yamanouchi Pharmaceutical Co., Ltd.)
来源:EP 0354806; US 4990503; US 5039669
合成路线图解说明:

The cyclization of 2-aminopyridine (I) with ethyl 4-bromoacetoacetate (II) by means of NaHCO3 in hot dioxane gives the imidazopyridine (III), which is hydrolyzed at the ester function with KOH in ethanol yielding the free acid (IV) . Finally, the treatment of acid (IV) with phosphorous acid and PCl3 in chlorobenzene at 115 C, followed by hydrolysis in boiling 6N HCl yielded the target bisphosphonate.

参考文献No.57762
标题:Novel preparation method of heterocyclic bis(phosphonic acid) derivs.
作者:Ishii, M.; Takaoka, K. (Yamanouchi Pharmaceutical Co., Ltd.)
来源:JP 1999269184
合成路线图解说明:

The cyclization of 2-aminopyridine (I) with ethyl 4-bromoacetoacetate (II) by means of NaHCO3 in hot dioxane gives the imidazopyridine (III), which is hydrolyzed at the ester function with KOH in ethanol yielding the free acid (IV) . Finally, the treatment of acid (IV) with phosphorous acid and PCl3 in chlorobenzene at 115 C, followed by hydrolysis in boiling 6N HCl yielded the target bisphosphonate.

参考文献No.477818
标题:Studies on novel bone resorption inhibitors. II. Synthesis and pharmacological activities of fused aza-heteroarylbisphosphonate derivatives
作者:Takeuchi, M.; Sakamoto, S.; Kawamuki, K.; Kurihara, H.; Nakahara, H.; Isomura, Y.
来源:Chem Pharm Bull 1998,46(11),1703
合成路线图解说明:

The cyclization of 2-aminopyridine (I) with ethyl 4-bromoacetoacetate (II) by means of NaHCO3 in hot dioxane gives the imidazopyridine (III), which is hydrolyzed at the ester function with KOH in ethanol yielding the free acid (IV) . Finally, the treatment of acid (IV) with phosphorous acid and PCl3 in chlorobenzene at 115 C, followed by hydrolysis in boiling 6N HCl yielded the target bisphosphonate.

参考文献No.582731
标题:Synthesis and pharmacological activity of imidazo-[1,2-a]pyridine-2-acetic and -2,3-dicarboxylic acid and related compounds
作者:Casagrande, C.; et al.
来源:Farmaco 1968,23(12),1141
合成路线图解说明:

The cyclization of 2-aminopyridine (I) with ethyl 4-bromoacetoacetate (II) by means of NaHCO3 in hot dioxane gives the imidazopyridine (III), which is hydrolyzed at the ester function with KOH in ethanol yielding the free acid (IV) . Finally, the treatment of acid (IV) with phosphorous acid and PCl3 in chlorobenzene at 115 C, followed by hydrolysis in boiling 6N HCl yielded the target bisphosphonate.

参考文献No.701186
标题:
作者:Atsumi, T.; et al.
来源:JP 7688965
合成路线图解说明:

This compound can be obtained by two related ways: 1) By cyclization of aminomalonamide (I) with ethyl orthoformate (II) at 150 C catalyzed with acetic acid. 2) By cyclization of (I) with ethyl formimidate (III) at 150 C catalyzed with acetic acid.

合成路线图解说明:

The cyclization of 2-aminopyridine (I) with ethyl 4-bromoacetoacetate (II) by means of NaHCO3 in hot dioxane gives the imidazopyridine (III), which is hydrolyzed at the ester function with KOH in ethanol yielding the free acid (IV) . Finally, the treatment of acid (IV) with phosphorous acid and PCl3 in chlorobenzene at 115 C, followed by hydrolysis in boiling 6N HCl yielded the target bisphosphonate.

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