新产品编号:1941623

Chemical Name: 3-[9-Amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6,7,1-hi]indol-3(S)-yl]-2-methyl-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidine-7-carboxylic acid methyl ester
项目整合开发状态: Biological Testing
项目研究机构: Jouveinal (Originator), Pfizer (Originator)
合成路线:3(R)-Amino-1-phenyl-6,7-dihydro-3H-[1,4]diazepin[6,7,1-hi]indol-4-one (I) was nitrated using KNO3 in concentrated H2SO4 to furnish the 9-nitro derivative (II).Coupling of (II) with 2-amino-6-(methoxycarbonyl)pyridine-3-carboxylic acid (III) in the presence of DCC and HOBt gave amide (IV).Imidate (V) was prepared by heating (IV) with trimethyl orthoacetate under vacuum distillation of the generated MeOH.Cyclization of (V) to produce the target pyridopyrimidine system (VI) was achieved using scandium triflate as the catalyst.The nitro group was finally hydrogenated over Ru/C to yield the title amino derivative.