- Efficient synthesis method of dipyridamole
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The invention discloses an efficient synthesis method of dipyridamole. The method comprises the following steps: dissolving a dichloro compound and diethanol amine into a solvent 1,3-dioxane to form ahomogeneous reactant; adding a catalyst, namely 001*7 strongly acidic cation exchange resin in the process of a reaction, wherein a reaction temperature is 75-80 DEG C, reaction time is 4-5 hours, and the content of a crude product reaches 95%; carrying out filtering to directly remove diethanol amine hydrochloride; filtering out the cation exchange resin by using a small bag filter, and washingand drying the cation exchange resin so as to recycling the cation exchange resin; drying a filtered crude product in a tray oven at 70-80 DEG C, recycling the solvent for indiscriminate usage, and adding ethanol accounting for 1.5 times of the weight of the dried crude product; carrying out heating to 78-80 DEG C, performing refluxing and dissolving, then conducting cooling to 15-20 DEG C, and performing crystallizing to obtain a finished product. The method is simple in process, beneficial for reducing energy consumption, safe and environment-friendly to operate, low in by-product amount, high in yield and convenient for industrial production.
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Paragraph 0006-0008
(2020/08/10)
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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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Paragraph 0007; 0017
(2018/06/04)
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- Preparation method for dipyridamole
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The invention belongs to the chemical field, and particularly relates to a preparation method for dipyridamole; diethanol amine and 2,6-dichloro-4,8-dipiperidinopyrimidino[5,4-D]pyrimidine are subjected to a reaction at relatively low temperature to generate dipyridamole, the dipyridamole crude product is subjected to secondary refining, and the yield and the chemical purity of the finally obtained dipyridamole are respectively increased to 94% or more and 98% or more; and the preparation method has the advantages of mild reaction, high reaction efficiency, low cost and the like, and is suitable for wide promotion and application.
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Paragraph 0027; 0028; 0029; 0030; 0031; 0032; 0033-0056
(2017/06/30)
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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 0038; 0039; 0040
(2017/08/31)
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- PROCESSES FOR THE PREPARATION OF DIPYRIDAMOLE
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The present invention relates to the active pharmaceutical ingredient dipyridamole. In particular, it relates to efficient processes for the preparation of dipyridamole which are amenable to large scale commercial production and provide the required product with improved yield and purity. The present invention also relates to a novel crystallization method for the purification of dipyridamole.
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Page/Page column 18; 19
(2011/12/14)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF DIPYRIDAMOLE
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The present invention relates to an improved process for the preparation of Dipyridamole of formula (I) by reacting 2,6-Dichloro-4, 8-dipiperidinopyrimido (5,4- d) pyrimidine (DDH) with Diethanolamine (DEA) using l-Methyl-2-pyrrolidinone (NMP) as a solvent.
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Page/Page column 4-6
(2008/06/13)
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- Use of radical-scavenging compounds for treatment and prevention of NO-dependent microcirculation disorders
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A method of treatment of the human or non-human animal body for treating NO-dependent microcirculation disorders is disclosed, for example microcirculation disorders caused by metabolic diseases, such as elevated levels of homocystin-homocystein inflammatory reactions or autoimmune diseases, furthermore peripheral microcirculation disorders or microcirculation disorders associated with increased cell fragmentation, which method comprises administering to a human or non-human animal body in need of such treatment an effective amount of a pharmaceutical composition containing a substance which scavenges free radicals, e.g. a pyrimido-pyrimidine selected from Dipyridamole, Mopidamol and the pharmaceutically acceptable salts thereof, and the use such substance for the manufacture of a corresponding pharmaceutical composition, optionally in combination with an agent capable of increasing NO procution.
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- Prodrugs for the therapy of tumors and inflammatory disorders
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Compounds of the formula Iglycosyl-Y[--C( Y)--X--] p --W(R) n --Z--C( Y)-active compound (I)are described which are suitable for the treatment of carcinomatous diseases, autoimmune diseases and chronic inflammatory diseases such as rheumatoid arthritis.
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- Structure-activity relationships of pyrimido-pyrimidine series of 5-lipoxygenase inhibitors
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A series of pyrimido-pyrimidine compounds were synthesized and a SAR study was conducted for 5-LO inhibition using a broken cell preparation from RBL-1 cells. In this series compound 21 was found to be a potent 5-LO inhibitor in vitro.
- Basha, Anwer,Ratajczyk, James D.,Dyer, Richard D.,Young, Patrick,Carter, George W.,Brooks, Clint D.W.
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- Pharmaceutical composition and process of treatment
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A process for alleviating proliferative skin diseases such as psoriasis, atopic dermatitis, etc. comprising administering to humans, or domesticated animals, topically and/or systemically a composition comprising a pharmaceutical carrier and at least one active compound selected from the groups, substituted alkyl zanthines, tricyclic antidepressants, organic nitrates, antihypertensives, anti-asthma agents and central nervous system depressants and combinations of certain compounds from specifically named groups of compounds.
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