PNU-167532
Chemical Name: 2-Benzyl-4-(3,4-difluorophenyl)-4-oxobutyric acid
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:Conjugate addition of benzylmagnesium chloride (II) to unsaturated ketone (I) in the presence of cuprous iodide-dimethyl sulfide complex afforded the 2-benzyl derivative (III).Then,the ester function was saponified with NaOH in MeOH to give the title acid.Resolution of the enantiomers was effected by fractional crystallization of the ephedrine salts.
📌 参考资料/链接:
参考文献标题:4-Phenyl-4-oxo-butanoic acid derivatives inhibitors of kynurenine 3-hydroxylase
文献作者:Giordani,A.; Pevarello,P.; Cini,M.; Bormetti,R.; Greco,F.; Toma,S.; Speciale,C.; Varasi,M.
参考来源:Bioorg Med Chem Lett 1998,8(20),2907