网站主页>>>
项目整合精选>>>
项目整合精选>>>Zoledronic acid monohydrate, CGP-42446(anhydrous), ZOL-446, CGP-42446A(disodium salt), CGP-42446B(triNa salt, hydrate), Zometa
Zoledronic acid monohydrate, CGP-42446(anhydrous), ZOL-446, CGP-42446A(disodium salt), CGP-42446B(triNa salt, hydrate), Zometa
唑来磷酸 唑来膦酸 唑来膦酸二钠盐四水合物Chemical Name: 1-Hydroxy-2-(1-imidazolyl)ethylene-1,1-diphosphonic acid monohydrate
CAS No. 165800-06-6, 118072-93-8 (anhydrous), 165800-07-7 (diNa salt), 157432-59-2 (Mg salt), 131654-46-1 (Na salt), 165800-08-8 (triNa salt, hydrate), 157432-58-1 (Zn salt)
项目整合开发状态: Launched-2000
项目研究机构: Novartis (Orphan Drug), Novartis (Originator)
合成路线: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.
📌 参考资料/链接：
参考文献标题:Substituted alkanediphosphonic acids and pharmaceutical use
文献作者:Jaeggi,K.A.; Widler,L.(Novartis AG)
参考来源:AU 8781453; EP 0275821; JP 1988150291; US 4939130
📄 详细内容
合成路线: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.
参考文献标题:Zoledronate Disodium
文献作者:Castar,J.; Rabasseda,X.; Sorbera,L.A.
参考来源:Drugs Fut 2000,25(3),259
合成路线: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.
参考文献标题:Highly potent geminal bisphosphonates.From pamidronate disodium (Aredia) to zoledronic acid (Zometa)
文献作者: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.
参考来源:J Med Chem 2002,45(17),3721