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项目整合精选>>>Bromfenac sodium, AHR-10282B, AHR-10282(anhydrous), Xibrom, Bronuck, Duract
Bromfenac sodium, AHR-10282B, AHR-10282(anhydrous), Xibrom, Bronuck, Duract
(2-氨基-3-(4-溴苯甲酰)苯基)乙酸钠 溴芬酸钠 2-(2-氨基-3-(4-溴苯甲酰基)苯)乙酸Chemical Name: 2-[2-Amino-3-(4-bromobenzoyl)phenyl]acetic acid monosodium salt sesquihydrate; 2-Amino-3-(4-bromobenzoyl)benzeneacetic acid monosodium salt sesquihydrate
CAS No. 120638-55-3, 91714-93-1 (anhydrous), 91714-94-2 (anhydrous, free acid)
项目整合开发状态: Launched-2000
项目研究机构: Wyeth Pharmaceuticals (Originator), GlaxoSmithKline (Licensee), ISTA Pharmaceuticals (Licensee), Senju (Licensee)
合成路线:The cyclization of 2-amino-4'-bromobenzophenone (I) with ethyl 2-(methylthio)acetate (II) by means of tert-butyl hypochlorite in dichloromethane at 70 C gives 7-(4-bromobenzoyl)-3-(methylthio)-2,3-dihydro-1H-indol-2-one (III),which is desulfurized by a treatment with Raney Nickel in THF yielding 7-(4-bromobenzoyl)-2,3-dihydro-1H-indol-2-one (IV).Finally,this compound is hydrolyzed with refluxing 3N NaOH and acidified with concentrated HCl.
📌 参考资料/链接：
参考文献标题:2-Aminophenylacetic acid derivs.
文献作者:Moran,H.W.; Welstead,W.J.Jr.(A.H.Robins Co.Inc.)
参考来源:US 4126635
📄 详细内容
合成路线:The cyclization of 2-amino-4'-bromobenzophenone (I) with ethyl 2-(methylthio)acetate (II) by means of tert-butyl hypochlorite in dichloromethane at 70 C gives 7-(4-bromobenzoyl)-3-(methylthio)-2,3-dihydro-1H-indol-2-one (III),which is desulfurized by a treatment with Raney Nickel in THF yielding 7-(4-bromobenzoyl)-2,3-dihydro-1H-indol-2-one (IV).Finally,this compound is hydrolyzed with refluxing 3N NaOH and acidified with concentrated HCl.
参考文献标题:Anti-inflammatory agents.3.Synthesis and pharmac
文献作者:Walsh,D.A.; Moran,H.W.; Shamblee,D.A.; Uwaydah,I.M.; Welstead,W.J.Jr.; Sancilio,L.F.; Dannenburg,W.N.
参考来源:J Med Chem 1984,27(11),1379-88
合成路线:The cyclization of 2-amino-4'-bromobenzophenone (I) with ethyl 2-(methylthio)acetate (II) by means of tert-butyl hypochlorite in dichloromethane at 70 C gives 7-(4-bromobenzoyl)-3-(methylthio)-2,3-dihydro-1H-indol-2-one (III),which is desulfurized by a treatment with Raney Nickel in THF yielding 7-(4-bromobenzoyl)-2,3-dihydro-1H-indol-2-one (IV).Finally,this compound is hydrolyzed with refluxing 3N NaOH and acidified with concentrated HCl.
参考文献标题:BROMFENAC SODIUM < Rec INNM; USAN >
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1988,13(11),943