- 2,6-bis(diethanolamine)-4,8-dipiperidine-pyrimidine-[5,4-d]pyrimidine synthetic method
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The invention discloses a 2,6-bis(diethanolamine)-4,8-dipiperidine-pyrimidine-[5,4-d]pyrimidine synthetic method. According to the invention, orotic acid is taken as an initial raw material, which iscompletely different with the raw material in the prior art, usage of diethanolamine is omitted, so that an end product as a uniform target product is obtained, the target product is shown as a formula I, and at the same time, the end product yield is increased so that the end product is economic and practical on industrial production.
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Paragraph 0030; 0034-0035
(2018/11/22)
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- Production method of dipyridamole bulk drug
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The invention provides a production method of a bulk drug of dipyridamole, which relates to the field of the synthesis of chemical bulk drugs. The production method comprises the following steps: protecting carbonyl of urea, performing condensation reaction with 2,3-diaminosuccinic acid, performing chlorination for hydroxyl of a condensation reactant, replacing chlorine with piperidine, hydrolyzing an obtained product, obtaining a compound containing two carbonyls, separating the product, enabling the separated product to have condensation reaction with diethanol amine, obtaining dipyridamole,and refining to obtain a finished product. By adopting the production method, the synthetic procedure of the dipyridamole is simplified, the conversion rate of raw materials can be greatly increased,and the production cost is decreased.
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- Novel technology with introduced catalyst to optimize synthesis of dipyridamole
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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.
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Paragraph 0028; 0029; 0030
(2017/08/31)
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