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项目整合精选>>>Alendronate sodium, Alendronic acid sodium salt, L-670452, MK-0217, GTH-42(diNa salt), G-704650(trihydrate), MK-217, AHButBP, AHBuBP, Fosamac, Bonalon, Teiroc(former Brand Name), Onclast, Alendros, Fosamax
Alendronate sodium, Alendronic acid sodium salt, L-670452, MK-0217, GTH-42(diNa salt), G-704650(trihydrate), MK-217, AHButBP, AHBuBP, Fosamac, Bonalon, Teiroc(former Brand Name), Onclast, Alendros, Fosamax
阿仑膦酸 阿仑膦酸钠,三水合物 Chemical Name: (4-Amino-1-hydroxybutylidene)bisphosphonic acid sodium salt
CAS No. 66376-36-1 (free acid), 121268-17-5 (triNa salt, trihydrate)
项目整合开发状态: Launched-1993
项目研究机构: Gentili (Originator), Abiogen (Not Determined), Banyu (Licensee), Merck & Co. (Licensee), Merck Frosst (Licensee), Merck Sharp & Dohme (Licensee), Teijin (Licensee)
合成路线:This compound has been obtained by three related ways:1) The reaction of 4-phthalimido butyryl chloride (I) with phosphorous acid at 130 C,followed by hydrolysis with refluxing 6N HCl gives the target phosphonic acid.2) The reaction of 4-phthalimido butyric acid (II) with phosphorous acid and phosphorous trichloride at 80 C,followed by hydrolysis with refluxing 48% HBr gives the target phosphonic acid.3) The reaction of 4-maleimido butyric acid (III) with phosphorous acid and phosphorous trichloride at 80 C,followed by hydrolysis with refluxing 48% HBr gives the target phosphonic acid.
📌 参考资料/链接:
参考文献标题:Novel process for preparing alendronic acid
文献作者:Lidor-Hadas,R.; et al.(Teva Pharmaceutical Industries Ltd.; Teva Pharmaceuticals USA,Inc.)
参考来源:WO 0049026