- A kind of avanafil impurity D and synthesis method and application thereof
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The present invention provides a new aphranarfil impurity and synthesis method thereof, by synthesizing and characterizing the impurity, the structure of the impurity is determined, the drug impurity profile of avanafil is perfected, the resulting product is of high purity, can be used as a control for drug quality control research.
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- Preparation method of avanafil impurity
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The invention discloses a preparation method of an avanafil impurity. The preparation method comprises the following steps: A) taking 4-(3-chloro-4-methoxyphenylamino)-5-ethoxycarbonyl-2-methylthio pyrimidine I as a raw material, and obtaining a compound
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- Method of preparing medical compound stendra
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The invention discloses a method of preparing a medical compound stendra and belongs to the technical field of medical compounds. The key point of the technical scheme is as follows: the synthetic route of the method of preparing the medical compound stendra is as follows: a formula as shown in the description. The method has the advantages of being high in yield, low in cost, economical and environment-friendly, suitable for industrialization, high in product impurity and the like, and is a synthetic method which has industrial production value.
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- Atorvastatin that non-preparation method
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The invention relates to a preparation method of avanafil and a new compound provided in a preparation process. According to the method, 5-uracil carboxylic acid or an ester thereof is taken as the raw material, and the avanafil meeting the clinical requirements can be synthesized at a relatively cost; besides, the preparation method is simple and convenient to operate, mild in reaction conditions, high in yield, low in cost, environmentally friendly and suitable for industrial large-scale production of the avanafil.
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- Method for preparing avanafil raw material medicine
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The invention relates to the technical field of medicine synthesis, and discloses a method for preparing an avanafil raw material medicine. The method comprises the following steps: taking a midbody -MI as an initial raw material, and performing an oxidation reaction, a condensation reaction with L-proline, a hydrolysis reaction and a dehydration condensation reaction in sequence, thereby obtaining avanafil. Aiming at the problems that a monitoring and analysis method of a conventional avanafil preparation method is not available, the invention provides a set of effective monitoring and detection method, the quality of middle products and final products can be effectively controlled, meanwhile due to adjusted purification methods of different steps, the purity of the middle products and the final products can be at a relatively high level, and the method is particularly applicable to industrial large-scale production.
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- A arab League cuts down that non-intermediate and its preparation method and application
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The invention discloses an avanafil intermediate as well as a preparation method and application thereof. The avanafil intermediate is a compound having a general formula as shown in the description, wherein R in the general formula is selected from C1-C4 alkyl. The preparation method of the intermediate comprises the steps a-d in the synthesis route as shown in the description. The invention also discloses an application of the intermediate. Each reaction step for preparing avanafil from the intermediate has the advantages of simple operation, mild reaction conditions, easily available reaction raw materials, high reaction yield and the like, the products are easy to separate and purify; the total yield of prepared avanafil is increased to 40% and the HPLC purity reaches up to 99.8%; the preparation cost of avanafil is greatly reduced, the quality of avanafil is ensured, and thus the intermediate is very much in line with industrial production requirements and has practical value.
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- BICYCLIC SUBSTITUTED PYRIMIDINE COMPOUNDS
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The present invention relates to the technical field of medicine and pharmacy, and particularly relates to bicyclic group substituted pyrimidine compounds represented by general formula (I), pharmaceutical acceptable salts thereof or stereoisomers thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification. The present invention also relates to preparation methods, pharmaceutical formulations, and pharmaceutical compositions of the compounds, and use of the compounds, pharmaceutical formulations, and pharmaceutical compositions for preparing a medicament for treating and/or preventing sexual dysfuntion diseases and diseases with lower urinay tract symptoms.
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- PROCESS FOR THE PREPARATION OF (S)-4-[(3-CHLORO-4-METHOXYBENZYL)AMINO]-2-[2- (HYDROXYMETHYL)-1-PYRROLIDINYL]-N-(2-PYRIMIDINYL METHYL-5-PYRIMIDINE CARBOXAMIDE
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The present invention relates to an improved process for the preparation of (S)-4-[(3- chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinyl ethyl)- 5-pyrimidine carboxamide compound of formula-1 represented by the following structural formula.
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- The discovery of avanafil for the treatment of erectile dysfunction: A novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor
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Novel pyrimidine-5-carboxamide derivatives bearing a 3-chloro-4-methoxybenzylamino group at the 4-position were identified as potent and highly selective phosphodiesterase 5 inhibitors. Among them, we successfully found 10j (avanafil) which exhibited a potent relaxant effect on isolated rabbit cavernosum (EC30 = 2.1 nM) and a high isozyme selectivity.
- Sakamoto, Toshiaki,Koga, Yuichi,Hikota, Masataka,Matsuki, Kenji,Murakami, Michino,Kikkawa, Kohei,Fujishige, Kotomi,Kotera, Jun,Omori, Kenji,Morimoto, Hiroshi,Yamada, Koichiro
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p. 5460 - 5465
(2015/01/08)
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- Preparations for oral administration
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The present invention provides a preparation for oral administration containing a medicinal substance having cGMP-specific phosphodiesterase inhibitory activity and showing decrease of solubility in the neutral and alkaline regions, wherein an acidic substance is compounded promote the dissolution of the medicinal substance in digestive tract and thus the efficacy can be expressed at the early stage after administration, and which preparation is useful in treatment of erectile dysfunction.
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- Aromatic nitrogen-containing 6-membered cyclic compounds
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An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R1 is a substituted or unsubstituted lower alkyl group, —NH—Q—R3 (R3 is a substituted or unsubstituted nitrogen containing heterocyclic group, and Q is a lower alkylene group or a single bond), or —NH—R4 (R4 is a substituted or unsubstituted cycloalkyl group); R2 is a substituted or unsubstituted aryl group; one of Y and Z is ═CH—, and the other is ═N—, or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent selective PDE V inhibitory activities, and hence, being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.
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- TABLETS QUICKLY DISINTEGRATED IN ORAL CAVITY
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Intraorally rapidly disintegrating tablets which, when ingested, disintegrates in the oral cavity rapidly without presenting unpleasant taste, can be quickly absorbed in the digestive tract and express efficacy are provided. The intraorally rapidly disintegrating tablets contain a drug being hardly water-soluble under neutral or alkaline conditions and being highly water-soluble under acidic conditions yet presenting unpleasant taste, which tablets can be prepared by combining the medicinal substance with a water-soluble acidic substance, coating either or both of the substances with a water-soluble coating agent being insoluble in alcoholic solvent, further adding a water-soluble binding agent being soluble in alcoholic solvent and a water-soluble saccharide, subjecting the resultant mixture to compression, and treating the products with an alcoholic solvent.
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