Flobufen, VUFB-16066
4-[4-(2,4-二氟苯基)苯基]-2-甲基-4-氧代丁酸 2,4-二氟-α-甲基-γ-氧-(1,1-双苯)-4-丁酸 Chemical Name: 4-(2',4'-Difluorobiphenylyl)-4-oxo-2-methylbutanoic acid; 3-[4-(2,4-Difluorophenyl)benzoyl]-2-methylpropionic acid; gamma-Oxo-(2',4'-difluoro-[1,1']biphenyl-4-yl)-2-methylbutanoic acid; 2',4'-Difluoro-alpha-methyl-gamma-oxo-[1,1'-biphenyl]-4-butanoic acid
CAS No. 112344-52-2, 104941-35-7 (former CAS)
项目整合开发状态: Phase III
项目研究机构: Res. Inst. Pharmacy Biochemistry (VUFB) (Originator)
合成路线:Flobufen is prepared by a Friedel-Crafts reaction of 2,4-difluorobiphenyl (II) with methylsuccinic anhydride (I).Methylsuccinic acid (III) can be obtained by hydrolysis and subsequent decarboxylation of ethyl 2-cyano-3-methylsuccinate (IV),which is prepared by condensation of ethyl ester of 2-bromopropionic acid (V) with ethyl cyanoacetate.2,4-Difluorobiphenyl (II) can be obtained by a Gomberg reaction of 2,4-difluorophenyl diazonium salt (VI) [prepared from difluoroaniline (VII)] with toluene in the presence of Cu.
📌 参考资料/链接：
参考文献标题:omega-(2',4'-Dihalobiphenylyl)oxoalkanoic acid derivs.
文献作者:Kuchar,M.; Brunova,B.; Grimova,J.; Maturova,E.(SPOFA - United Pharmaceutical Works)
参考来源:CS 243570; EP 0180290; JP 1986065842; US 4683331
📄 详细内容
合成路线:Flobufen is prepared by a Friedel-Crafts reaction of 2,4-difluorobiphenyl (II) with methylsuccinic anhydride (I).Methylsuccinic acid (III) can be obtained by hydrolysis and subsequent decarboxylation of ethyl 2-cyano-3-methylsuccinate (IV),which is prepared by condensation of ethyl ester of 2-bromopropionic acid (V) with ethyl cyanoacetate.2,4-Difluorobiphenyl (II) can be obtained by a Gomberg reaction of 2,4-difluorophenyl diazonium salt (VI) [prepared from difluoroaniline (VII)] with toluene in the presence of Cu.
参考文献标题:FLOBUFEN
文献作者:Rejholec,V.
参考来源:Drugs Fut 1989,14(1),24
产品链接: CAS No. 112344-52-2›› 产品链接: CAS No.104941-35-7››