PD-165167
Chemical Name: 7-[N-[2-(Phenylamino)ethyl]aminomethyl]-2H-[1]benzopyran-2-one
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Photochemical bromination of 7-methylcoumarin (I) using N-bromosuccinimide and azobis(isobutyronitrile) provided the benzylic bromide (II).N-Phenyl ethylenediamine (V) was prepared by reaction between aniline (III) and oxazolidone (IV) at 140 C.Then,alkylation of amine (V) with bromide (II) in the presence of K2CO3 in refluxing acetonitrile provided the title compound.
📌 参考资料/链接：
参考文献标题:Design,synthesis,and evaluation of coumarins as potent and selective dopamine D4 antagonists
文献作者:Kesten,S.R.; et al.
参考来源:216th ACS Natl Meet (Aug.23-27,Boston) 1998,Abst MEDI 123
📄 详细内容
合成路线:Photochemical bromination of 7-methylcoumarin (I) using N-bromosuccinimide and azobis(isobutyronitrile) provided the benzylic bromide (II).N-Phenyl ethylenediamine (V) was prepared by reaction between aniline (III) and oxazolidone (IV) at 140 C.Then,alkylation of amine (V) with bromide (II) in the presence of K2CO3 in refluxing acetonitrile provided the title compound.
参考文献标题:Design,synthesis,and evaluation of chromen-2-ones as potent and selective human dopamine D4 antagonists
文献作者:Kesten,S.R.; Heffner,T.G.; Johnson,S.J.; Pugsley,T.A.; Wright,J.L.; Wise,L.D.
参考来源:J Med Chem 1999,42(18),3718