330786-34-0Relevant articles and documents
Method for synthesizing avanafil impurities
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Paragraph 0029-0031; 0036-0041, (2021/04/17)
The invention discloses a method for synthesizing avanafil impurities, which belongs to the field of drug synthesis and has the advantages of reasonable process design, strong operability and mild reaction conditions. The preparation method comprises the following steps: A. hydrolyzing 4-(3-chlorine-4-methoxy phenylamino)-5-ethoxy carbonyl-2-methylthio pyrimidine I serving as a raw material in the presence of alkali to obtain a compound II; B, condensing the compound II and 2-aminomethylpyrimidine hydrochloride III under an alkaline condition to obtain a compound IV; C, oxidizing the compound IV in the presence of an oxidant to obtain a compound V; and D, reacting the compound V under an alkaline condition to obtain the avanafil impurity VI. According to the avanafil impurity prepared by the method, the impurity spectrum of avanafil is perfected, an important basis is provided for quality research of avanafil, and the safety of avanafil is further improved through research and control of the impurity.
A process for the preparation of atorvastatin that non-intermediate and its preparation method
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Paragraph 0039; 0040; 0041; 0056-0058; 0072-0074; 0088-0090, (2017/08/25)
The invention provides a novel intermediate IV which is used for preparation of avanafil. The intermediate has a general formula IV as described in the specification; and in the general formula IV, R represents a C1-20 alkylsulfinyl group or a C1-20 alkylsulfonyl group. The intermediate has high purity, is suitable for industrial production and can be subjected to a one-step chemical reaction to prepare avanafil. The invention also provides a preparation method for the intermediate and a method for preparing avanafil from the intermediate.
8-(3-Chloro-4-methoxybenzyl)-8H-pyrido[2,3-d]pyrimidin-7-one derivatives as potent and selective phosphodiesterase 5 inhibitors
Sakamoto, Toshiaki,Koga, Yuichi,Hikota, Masataka,Matsuki, Kenji,Mochida, Hideki,Kikkawa, Kohei,Fujishige, Kotomi,Kotera, Jun,Omori, Kenji,Morimoto, Hiroshi,Yamada, Koichiro
, p. 1431 - 1435 (2015/03/30)
A novel series of highly selective phosphodiesterase 5 (PDE5) inhibitors was found. 8H-Pyrido[2,3-d]pyrimidin-7-one derivatives bearing an (S)-2-(hydroxymethyl)pyrrolidin-1-yl group at the 2-position and a 3-chloro-4-methoxybenzyl group at the 8-position