The invention discloses a novel technology with an introduced catalyst to optimize the synthesis of
dipyridamole, and belongs to the technical field of medical intermediates. According to the technology, in the step of oxidizing a
methyl group of 6-methyl
uracil into
formic acid, a Co(OAc)2 / HOAc / AIBN / O2 catalytic
system is introduced, and the reaction yield is increased to 90 to 95%. In the step of reducing a nitro group of nitro-
orotic acid into an amino group, activated
copper powder is taken as the catalyst, the yield is more than 85%; and moreover, the environmental
pollution and danger caused by
sodium hydrosulfite are avoided. In the step of converting substituted hydroxyl group into substituted
chlorine, SOCl12 and N,N-
dimethyl formamide are introduced into the
reaction system so as to reduce the environment
pollution and the difficulty of
post treatment. In the reactions of preparing 2,6-dichloro-4,8-bis(
piperidine-1-yl)pyrimido[5,4-d]
pyrimidine from perchloro pyrimido[5,4-d]
pyrimidine, a CuI / PhNO2 catalytic
system is introduced into the
reaction system, the reaction yield reaches 95%, moreover, the operation is easy, and the treatment is simple. The provided technology increases the yield, reduces the cost, guarantees the safety, saves the energy, and meets the requirements of green reactions and modern
chemical production.