- Preparation method and application of Nafamostat mesylate intermediate
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The invention belongs to the field of intermediate preparation and particularly relates to a preparation method and the application of a Nafamostat mesylate intermediate. The preparation method of theNafamostat mesylate intermediate comprises the step of enabling o/p-aminobenzoic acids to react with cyanamide under the action of a catalyst in a solvent, wherein the catalyst is hydrochloric acid ethanol or hydrochloric acid methanol and preferably selects the hydrochloric acid ethanol. The invention further provides a method for further preparing a Nafamostat mesylate impurity standard productby utilizing the method. With the adoption of the preparation method of the Nafamostat mesylate intermediate, the reaction time is shortened, the reaction yield is improved, and the production cost and the storage pressure are reduced. Therefore, implementation values and social economic benefits are greater. Moreover, impurities in the Nafamostat mesylate production are qualitatively and quantitatively analyzed by the impurity standard product, so that the quality standard of the product can be improved, and an important guiding significance is provided for safe medication.
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Paragraph 0047-0051
(2019/10/23)
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- Synthetic method for N-guanidine hydrochloride
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The invention provides a synthetic method for N-guanidine hydrochloride. lime nitrogen is directly adopted for making a reaction without using hydrogen cyanamide, the problem about the stability of the hydrogen cyanamide is avoided, raw materials which are cheaper are easier to obtain are used, and reaction operation is simple.
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Paragraph 0023-0037
(2017/05/20)
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- Cleavage of 2-(Arylamino)-4,6-dimethoxypyrimidines to yield arylguanidines
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A novel method for the synthesis of aryl-substituted guanidines in good overall yields is presented; it consists of the acidic cleavage of 2-(arylamino)-4,6-dimethoxypyrimidines, which were prepared by coupling aryl bromides with 2-amino-4,6-dimethoxypyrimidine. This methodology introduces a new means of protection for the guanidine functionality. Copyright
- Shaw, Julian W.,Grayson, David H.,Rozas, Isabel
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p. 3565 - 3569
(2014/06/23)
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- FUSED HETEROCYCLYC INHIBITOR COMPOUNDS
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The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound
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Page/Page column 62
(2010/03/02)
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- Methods and compositions for treating or preventing bacterial infection
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The invention relates to compositions and methods for treating or preventing disease or disorders caused by or associated with certain bacterial infection, especially Escherichia coli (E. coli) or Helicobacter pylori (H. pylori) infection.
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- Synthesis of 4-(4-guanidinobenzoyloxy)benzamides and 1-(4-guanidinobenzoyloxy)benzoyloxy acetamides as trypsin inhibitors
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Seventeen new compounds of 4-(4-guanidinobenzoyloxy)benzamides and 4-(4-guanidinobenzoyloxy)benzoyloxyacetamides were prepared and their inhibitory activities on trypsin, thrombin and porcine pancreatic elastase were measured. These compounds were found to be selective trypsin inhibitors with inhibiting activities from 0.44 to 43 μM.
- Zlatoidsky,Maliar
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p. 895 - 899
(2007/10/03)
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- Anti-thrombotic peptide and pseudopeptide derivatives
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Disclosed are novel peptide and pseudopeptide derivatives and pharmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.
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