- Synthetic method of 1H-pyrazolo[3,4-d]pyrimidine-4-ol
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The invention discloses a synthetic method of 1H-pyrazolo[3,4-d]pyrimidine-4-ol. According to the method, triethyl orthoformate, morpholine and cyanoacetamide are used as basic raw materials, a solvent acetonitrile medium is replaced, 2-cyan-3-morpholine acrylamide is synthesized, the use of a traditional highly acid sulfuric acid raw material is abandoned, and organic acid is used as a catalyst to replace sulfuric acid. The original traditional three-step synthesis process is simplified to two-step process, and the synthesis route is shortened. Then, raw material cost is reduced, and the operation is simplified. By the synthetic method, product yield is increased, and generation of ''three wastes (waste gas, waste water and industrial residue) '' is reduced.
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Paragraph 0024; 0027-0028; 0033; 0036; 0039; 0042
(2018/11/27)
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- Synthetic method of allopurinol
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The invention relates to a synthetic method of allopurinol. The synthetic method comprises the following steps: (1) adding methyl cyanoacetate, triethyl orthoformate and ethyl acetic anhydride into areaction kettle, and stirring and heating for reflux, so as to obtain red brown alpha-ethoxylated methyl cyanoacetate; (2) adding absolute ethyl alcohol and hydrazine hydrate into the reaction kettle,heating for reflux, cooling for crystallization, and filtering, so as to obtain a crystal 3-amino-4-methoxycarbonyl pyrazole; (3) adding 3-amino-4-methoxycarbonyl pyrazole and formamide into the reaction kettle, stirring for reaction, and cooling for crystallization, so as to obtain crude allopurinol; and (4) adding an acid liquid into the reaction kettle, adding crude allopurinol and activated carbon, carrying out suction filtration while the liquid is hot, and carrying out low-temperature crystallization, so as to obtain allopurinol. The method is simple in process, the yield and purity ofthe product are effectively increased, the energy consumption is low in the reaction process, the environmental pollution is low, the raw materials are easily available, the price of allopurinol is low, the quality of the allopurinol is controllable, and an allopurinol finished product meets the standards of 2015 edition of the Pharmacopoeia and is suitable for industrial production.
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Paragraph 0005; 0028-0029; 0032-0033; 0036-0037; 0040-0041
(2018/03/01)
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- Efficient synthesis of14C-labeled 1H-pyrazolo[3,4-d]pyrimidine and related [4.3.0]-bicyclic pyrimidino systems
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In support of a research program aimed at discovering purine-related anticancer drug candidates, a method for the 14C-labeling of pyrazolopyrimidines utilizing the readily available labeled starting material, sodium [14C]formate, has been developed with a good overall yield. This new method was proven to be general in the preparation of other related [4.3.0]heterocycles containing N, O, and S atoms. A concise synthesis of a model compound, 8-aza-7-deaza-5′-[14C]noraristeromycin, was achieved utilizing this methodology as a key step.
- Ho, Jonathan Z.,Van Arsdale, Kyle R.,Braun, Matthew P.
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scheme or table
p. 958 - 963
(2009/03/11)
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- INHIBITORS OF Akt ACTIVITY
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Invented are novel thiophene compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 181
(2010/11/27)
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- PROCESS FOR PRODUCING PYRIMIDIN-4-ONE COMPOUND
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A pyrimidin-4-one compound can be prepared in a high yield by reacting an aminoarylcarboxylic acid compound with an organic acid compound in the presence of a nitrogen atom-containing compound under relatively simple and moderate reaction conditions.
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Page/Page column 10
(2008/06/13)
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- Process and device for producing liquid dosage formulations of medicinal compounds on demand from tablets and capsules
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The present invention provides a process for preparing liquid pharmaceutical formulations on demand from tablets and capsules.
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- 3-Chlor-5-dimethylamino-2-formyl-4-aza-2,4-pentadiennitril, Synthese und Umsetzungen mit Nucleophilen
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3-Chloro-5-dimethylamino-2-formyl-4-aza-2,4-pentadienenitrile (7) is prepared by partial hydrolysis of the iminium perchlorate 1.In 7 the electrophilic centres (1, 3, 5) regioselectively react with secondary alkylamines, arylamines, and hydrazine derivatives to yield 3-amino-substituted formylazapentadienenitriles and (hydrazonomethyl)azapentadienenitriles.Intramolecular cyclisation leads to triazole betaines, pyrazoles, and 1,4-dihydropyrimidines.
- Klemm, Kurt,Pruesse, Wolfgang,Baron, Lothar,Daltrozzo, Ewald
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p. 2001 - 2018
(2007/10/02)
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