新产品编号:2471593
Chemical Name: 2-(4-Chlorophenyl)-3-[4-(methylsulfonyl)phenyl]-4-oxo-2-pentenoic acid sodium salt
项目整合开发状态: Preclinical
项目研究机构: Merck Frosst (Originator)
合成路线:Condensation between 4-methylsulfonyl-2'-bromopropiophenone (I) and 4-chlorophenylacetic acid (II) in the presence of Et3N/DBU,followed by air oxidation,gives rise to the furanone derivative (III) (1).This is subsequently hydrolyzed with ethanolic NaOH to produce the title keto carboxylate compound (1,2).
📌 参考资料/链接：
参考文献标题:Diaryl-5-oxygenated-2-(5H)-furanones as COX-2 inhibitors
文献作者:Black,C.; Grimm,E.; Wang,Z.; Leger,S.(Merck Frosst Canada Inc.)
参考来源:EP 0828724; JP 1999505534; US 5691374; WO 9636623
📄 详细内容
合成路线:Condensation between 4-methylsulfonyl-2'-bromopropiophenone (I) and 4-chlorophenylacetic acid (II) in the presence of Et3N/DBU,followed by air oxidation,gives rise to the furanone derivative (III) (1).This is subsequently hydrolyzed with ethanolic NaOH to produce the title keto carboxylate compound (1,2).
参考文献标题:3,4-Diaryl-5-hydroxyfuranones: Highly selective inhibitors of cyclooxygenase-2 with aqueous solubility
文献作者:Black,W.C.; Brideau,C.; Chan,C.-C.; Charleson,S.; Cromlish,W.; Gordon,R.; Grimm,E.L.; Hughes,G.; Leger,S.; Li,C.-S.; Riendau,D.; Therien,M.; Wang,Z.; Xu,L.-J.; Prasit,P.
参考来源:Bioorg Med Chem Lett 2003,13(6),1195