1315478-16-0Relevant articles and documents
Method for preparing Fimasartan
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Paragraph 0040; 0041, (2019/01/16)
The invention discloses a method for preparing Fimasartan. The method comprises the steps that valeronitrile is used as a raw material to prepare pentanimidamide hydrochloride, then pentanimidamide hydrochloride and acetylsuccinic acid diethyl ester conduct a cyclization reaction and an amidation reaction to prepare 2-(2-normal-butyl-4-hydroxyl-6-methylpyrimidine-5-radical)-N,N-dimethylacetamide (intermediate II), the intermediate II is subjected to sulfo-carbonylation through a Lawesson's reagent to obtain 2-(2-normal-butyl-4-hydroxyl-6-methylpyrimidine-5-radical)-N,N-dimethylacetamide (intermediate III), the intermediate III is subjected to an N-alkylation reaction, radicals are protected through detritylation, and Fimasartan is prepared. The preparation method has the advantages of highreaction selectivity, high synthesis yield, high reaction efficiency and the like.
NOVEL PREPARATION METHOD OF 2-(2-N-BUTYL-4-HYDROXY-6-METHYL-PYRIMIDIN-5-YL)-N,N-DIMETHYLACETAMIDE
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Page/Page column 9, (2011/08/08)
The present invention provides a method for preparing 2-(2-n-butyl-4-hydroxy-6-methyl-pyrimidin-5-yl)-N,N-dimethylacetamide, comprising reacting a compound of the following formula 2 with pentanamidine or a salt thereof in the presence of a base. [Formula 2] wherein R1 represents C1-C6 linear or branched alkyl or C3-C6 cycloalkyl. Further, the present invention provides a method for preparing 2-(2-n-butyl-4-hydroxy-6-methyl-pyrimidin-5-yl)-N,N-dimethylacetamide, comprising the steps of: a) reacting 2-(2-n-butyl-4-hydroxy-6-methyl-pyrimidin-5-yl)-acetic acid with a haloformate compound in the presence of a base, and b) reacting the product of Step a) with dimethylamine.