【药物名称】Zoledronic acid monohydrate, CGP-42446(anhydrous), ZOL-446, CGP-42446A(disodium salt), CGP-42446B(triNa salt, hydrate), Zometa
化学结构式(Chemical Structure):
参考文献No.8718
标题:Substituted alkanediphosphonic acids and pharmaceutical use
作者:Jaeggi, K.A.; Widler, L. (Novartis AG)
来源:AU 8781453; EP 0275821; JP 1988150291; US 4939130
合成路线图解说明:

Zoledronate sodium can be prepared by reaction of 2-(1-imidazolyl)acetic acid hydrochloride (I) with PCl3, with optional presence of phosphoric acid, in refluxing chlorobenzene, followed by hydrolysis with refluxing 9N hydrochloric acid and final formation of the sodium salt by treatment with aqueous NaOH.

参考文献No.569207
标题:Zoledronate Disodium
作者:Casta馿r, J.; Rabasseda, X.; Sorbera, L.A.
来源:Drugs Fut 2000,25(3),259
合成路线图解说明:

Zoledronate sodium can be prepared by reaction of 2-(1-imidazolyl)acetic acid hydrochloride (I) with PCl3, with optional presence of phosphoric acid, in refluxing chlorobenzene, followed by hydrolysis with refluxing 9N hydrochloric acid and final formation of the sodium salt by treatment with aqueous NaOH.

参考文献No.685856
标题:Highly potent geminal bisphosphonates. From pamidronate disodium (Aredia) to zoledronic acid (Zometa)
作者:Widler, L.; Jaeggi, K.A..; Glatt, M.; Muller, K.; Bachmann, R.; Bisping, M.; Born, A.R.; Cortesi, R.; Guiglia, G.; Jeker, H.; Klein, R.S.; Ramseier, U.; Schmid, J.; Schreiber, G.; Seltenmeyer, Y.; Green, J.R.
来源:J Med Chem 2002,45(17),3721
合成路线图解说明:

Zoledronate sodium can be prepared by reaction of 2-(1-imidazolyl)acetic acid hydrochloride (I) with PCl3, with optional presence of phosphoric acid, in refluxing chlorobenzene, followed by hydrolysis with refluxing 9N hydrochloric acid and final formation of the sodium salt by treatment with aqueous NaOH.

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