- 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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Paragraph 0105-0107
(2018/03/24)
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- Sedinafine derivatives of the microwave-assisted method for preparing
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The invention discloses a microwave-assisted synthesis method of sildenafil derivatives, which mainly comprises the following steps: by using 2-alkoxybenzoic acid and 4-amino-1-methyl-3-n-propyl-1H-pyrazolyl-5-formamide as initial raw materials, carrying out amidation, cyclization, mononitration, nitro reduction, guanidylation and the like to obtain the sildenafil derivatives. The method greatly shortens the reaction time, enhances the reaction efficiency, has the advantages of high yield and high purity, is simple to operate and easy to control, and is beneficial to industrial production of sildenafil analogs.
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- PYRAZOLOPYRIMIDINETHIONE DERIVATIVES, SALTS AND SOLVATES THEREOF, PREPARATION METHODS AND USE THEREOF
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The present invention disclosed the pyrazolopyrimidinethione derivatives, salts and solvates thereof, preparation methods and use thereof. The pyrazolopyrimidinethione derivatives according to the present invention possess the structure of general formula I , wherein, R1, R2, R3, and R4 represent alkyl, alkenyl, or aryl; R5 represents hydrogen, alkyl, alkenyl, alkoxy, cycloalkyloxy, aryl, or alkylacyl; and R6 represents hydrogen, alkyl, alkenyl, cycloalkyloxy, or alkylacyl. The pharmaceuticals containing the compound of the present invention and used for the treatment of impotence and sexlessness have the advantages of high selectivity over PDEV, long action time, and less side reactions, and the pharmaceuticals will arouse no side reactions of blood pressure decreasing and heart rate increasing, and it has broad market propect.
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- Method of treating a patient having precancerous lesions with phenyl purinone derivatives
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Derivatives of Phenyl Purinone are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit growth of neoplastic cells.
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- PYRAZOLOPYRIMIDINONE ANTIANGINAL AGENTS
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Compounds of the formula:wherein R1 is H, C1-C3 alkyl, C3-C5 cycloalkyl or C1-C3 perfluoroalkyl; R2 is H, C1-C6 alkyl optionally substituted by OH, C1-C3 alkoxy or C3-C6 cycloalkyl, or C1-C3 perfluoroalkyl; R3 is C1-C6 alkyl, C3-C6 alkenyl, C3-C6 alkynyl, C3-C7 cycloalkyl, C1-C6 perfluoroalkyl or (C3 -C6 cycloalkyl)C1-C6 alkyl; R4 taken together with the nitrogen atom to which it is attached completes a pyrrolidinyl, piperidino, morpholino, or 4-N-(R6)-piperazinyl group; R5 is H, C1-C4 alkyl, C1-C3 alkoxy, NR7 R8, or CONR7 R8 ; R6 is H, C1-C6 alkyl, (C1-C3 alkoxy) C2-C6 alkyl, hydroxy C2-C6 alkyl, (R7 R8 N)C2 -C6 alkyl, (R7 R8 NCO)C1-C6 alkyl, CONR7 R8, CSNR7 R8 or C(NH)NR7 R8 ; R7 and R8 are each independently H, C1-C4 alkyl, (C1-C3 alkoxy)C2-C4 alkyl or hydroxy C2-C4 alkyl; and pharmaceutically acceptable salts thereof, are selective cGMP PDE inhibitors useful in the treatment of cardiovascular disorders such as angina, hypertension, heart failure and atherosclerosis
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- Pyrazolopyrimidinone antianginal agents
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Compounds of the formula STR1 and pharmaceutically acceptable salts thereof are selective cGMP PDE inhibitors which are useful in the treatment of such diseases and adverse conditions as angina, hypertension, congestive heart failure, reduced blood vessel patency, peripheral vascular disease, stroke, bronchitis, chronic asthma, allergic asthma, allergic rhinitis, glaucoma, and diseases characterized by disorders of gut motility.
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