330785-82-5Relevant academic research and scientific papers
A kind of avanafil impurity D and synthesis method and application thereof
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Paragraph 0017; 0021, (2022/01/12)
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.
Preparation method of avanafil impurity
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Paragraph 0031-0033; 0039-0042, (2021/05/19)
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
Preparation method of avanafil intermediate
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Paragraph 0025; 0037; 0038; 0041-0052, (2018/11/03)
The invention provides a preparation method of an avanafil intermediate. The preparation method comprises the following steps: dissolving a starting raw material 4-(3-chloro-4-methoxybenzylamino)5-ethoxycarbonyl-2-methylthiopyrimidine in a reaction solven
Method for preparing avanafil raw material medicine
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Paragraph 0047; 0063; 0064; 0065, (2017/08/28)
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.
Prodrugs Of Bicyclic Substituted Pyrimidine Type PDE-5 Inhibitors
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Paragraph 0206; 0207, (2016/03/13)
Provided are prodrugs of a bicyclic substituted pyrimidine type PDE-5 inhibitors, pharmaceutically acceptable salts or stereoisomers thereof. Also provided are methods for preparing these prodrug compounds, pharmaceutical preparations, and pharmaceutical compositions, as well as a use of these compounds, pharmaceutical preparations and pharmaceutical compositions in the manufacture of medicaments for treatment and/or prophylaxis of sexual dysfunction and lower urinary tract symptoms.
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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Page/Page column 26; 27, (2015/01/16)
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.
BICYCLIC SUBSTITUTED PYRIMIDINE COMPOUNDS
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Paragraph 0469; 0470, (2015/07/02)
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.
Cyclic compounds
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, (2008/06/13)
1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, —O—, —CH═N—, —N═CH—, —N═N—, —CH═CH—, etc., R1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R3 and a substituent in Y may be combined to form a lactone ring. The compound of the present invention has excellent selective PDE V inhibitory activity and therefore, is useful as a therapeutic or prophylactic drug for treating various diseases due to functional disorders on cGMP-signaling.
TABLETS QUICKLY DISINTEGRATED IN ORAL CAVITY
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Page 19, (2008/06/13)
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.
Aromatic nitrogen-containing 6-membered cyclic compounds
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, (2008/06/13)
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.
