Ro-09-3024

Chemical Name: 5-[N-(6,6-Dimethyl-2,4-heptadiynyl)-N-methylamino]-1,2,3,4-tetrahydroquinolin-2-one
项目整合开发状态: Preclinical
项目研究机构: Chugai (Originator)
合成路线:The Wittig reaction of 2,6-dinitrobenzaldehyde (I) with (ethoxycarbonylmethylene)triphenylphosphorane (A) produced methyl 2,6-dinitrocinnamate (II).Hydrogenation of the nitro groups and the olefinic double bond of (II) with concomitant cyclization furnished the tetrahydroquinolinone (III).Reductive alkylation of (III) with 6,6-dimethylheptadiynal (IV) and sodium cyanoborohydride produced the secondary amine (V).Finally,the N-methyl group was introduced by a second reductive alkylation with formaldehyde.