- Preparation method for heterocyclic compounds
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The invention specifically relates to a preparation method for heterocyclic compounds with udenafil as a representative, belonging to the field of chemical pharmaceutical technology. The invention aims to overcome the technical problems of high production cost, low yield, great treatment quantities of waste acid and exhaust gas and potential safety hazards in conventional synthetic methods. To overcome the technical problems, the invention provides the preparation method for the heterocyclic compounds. The preparation method comprises the following steps: 1, subjecting a starting raw materialA to a reaction under the action of an organic solvent and alkali to produce an intermediate 1; 2, reacting the intermediate 1 with a sulfonating agent to produce an intermediate 2; and 3, reacting the intermediate 2 with a starting raw material B in an organic solvent to obtain a finished compound as shown in a formula I. The preparation method provided by the invention uses easily available andcheap raw materials, avoids usage of expensive coupling reagents, improves the selectivity of next-step sulfonation, and is high in product yield and purity, mild in reaction conditions and beneficialfor scaled-up production in workshops.
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- PHARMACOLOGICAL COMPOSITION FOR PREVENTION AND TREATMENT OF RESPIRATORY DISEASE CONTAINING PYRAZOLOPYRIMIDINONE COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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Disclosed herein is composition for prevention and treatment of respiratory disease containing a pyrazolopyrimidinone compound or pharmaceutically acceptable salts thereof as an active ingredient.
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Page/Page column 6
(2010/04/03)
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- HIGHLY SELECTIVE and LONG-ACTING PDE5 MODULATORS
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Disclosed herein are substituted phosphodiesterase type 5 enzyme modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 59
(2008/12/07)
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- AGENT FOR THE PREVENTION AND TREATMENT OF LIVER DISEASES CONTAINING PYRAZOLOPYRIMIDINE DERIVATIVE
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The present invention relates to the pharmaceutical compositionfor prevention and treatment of liver diseases containing pyrazolopyrimidine derivative as an active ingredient. According to the present invention, pyrazolopyrimidine derivative has an excellent effect on inhibiting collagen synthesis in hepatic stellate cellsand acts directly on the portal vein. Particularly, it may increase the diameter and the amount of blood flow of the portal vein, and finally decrease the pressure thereof. Therefore, pyrazolopyrimidine derivative can be used advantageously for prevention and treatment of hepatic fibrosis, liver cirrhosis caused by hepatic fibrosis, portal hypertension and various complications caused by portal hypertension. In addition, pyrazolopyrimidine derivative according to the present invention can reduce dosing frequency because of its long half-life, and therefore, has an advantage to improve the drug compliance of patients suffering from chronical liver diseases.
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