新产品编号:1504991

Chemical Name: N-(Cyclopropylmethyl)-N-[2-methyl-8-(2,4,6-trimethylphenyl)quinolin-4-yl]-N-propylamine
项目整合开发状态: Preclinical
项目研究机构: Janssen (Originator), Neurocrine Biosciences (Originator)
合成路线:Suzuki coupling of 2-bromoaniline (I) with boronic acid (II) in the presence of a palladium catalyst gave biphenyl (III).Subsequent condensation of (III) with ethyl acetoacetate (IV) afforded enamine (V),which was cyclized to hydroxyquinoline (VI) in refluxing diphenyl ether.Chlorination of (VI) in boiling POCl3 produced the corresponding 4-chloroquinoline (VII).This was finally condensed with N-(cyclopropylmethyl)-N--propylamine (VIII) to provide the target aminoquinoline.