161718-81-6Relevant articles and documents
Preparation method of febuxostat intermediate
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Paragraph 0032; 0038-0070, (2021/11/10)
The invention belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of an important febuxostat intermediate. The preparation method comprises the following steps of: by taking dimethyl 4-isobutoxy isophthalate as a raw material, carrying out ammonolysis on ester groups under the action of a catalyst to obtain acylamino, and further dehydrating the acylamino to obtain 4-isobutoxybenzene-1, 3-dinitrile. According to the method, cyano groups are introduced in ammonolysis and dehydration modes, cyanide with high toxicity is avoided, a traditional catalyst is replaced with a green catalyst, the reaction is milder, economical and environmentally friendly, the yield is high, and the method is suitable for industrial production.
Preparation method and use of 2-phenyl-1,6-dihydropyrimidine-5-carboxylic acid derivative
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Paragraph 0076-0077; 0079-0080, (2019/09/14)
The invention belongs to the technical field of medicines, and relates to a preparation method and a use of a 2-phenyl-1,6-dihydropyrimidine-5-carboxylic acid derivative. The invention provides the 2-phenyl-1,6-dihydropyrimidine-5-carboxylic acid derivative represented by general formula I, or a pharmaceutically acceptable salt, an isomer, a polymorph and a medicinal solvate thereof, and further provides an intermediate for preparing the 2-phenyl-1,6-dihydropyrimidine-5-carboxylic acid derivative or the pharmaceutically acceptable salt thereof. The structure of the intermediate is representedby general formula II, III or IV; and in the formulas, R, R and R are as defined in claims and the description.
PROCESS FOR THE PREPARATION OF 2-[3-CYANO-4-(2-METHYLPROPOXY)PHENYL]-4-METHYLTHIAZOLE-5-CARBOXYLIC ACID AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
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, (2011/12/02)
The present invention relates to novel and improved processes for the preparation of 2-[3-cyano-4-(2-methylpropoxy) phenyl]-4-methylthiazole-5-carboxylic acid compound of formula-1 and its pharmaceutically acceptable salts thereof. the present invention also provides the novel process for the preparation of crystalline forms of 2-[3-cyano-4-(2-methylpropoxy) phenyl]-4-methylthiazole-5-carboxylic acid compound of formula-1 and its intermediates.