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.