cas 247257-48-3, 2-Butyl-5-dimethylaminothiocarbonylmethyl-6-methyl-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidin-4(3H)-one

Articles about 247257-48-3Total 5 be found

Process for Preparation of Fimasartan and Intermediate for Preparing the Same
The present invention relates to a simple and economically process for preparing fimasartan and its preparation intermediates. (by machine translation)
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(2020/10/20)

Method for preparing Fimasartan
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.
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(2019/01/16)

Method for synthesizing Fimasartan
The invention discloses a method for synthesizing Fimasartan. The method comprises the steps: subjecting a compound VI and a compound VII to a reaction in toluene, so as to obtain a compound V; subjecting the compound V and pentamidine hydrochloride to a reaction in the presence of alkali metal hydroxide, so as to obtain a compound IV; subjecting the compound IV to hydrogen drawing with lithium hydride in a mixed solvent prepared from toluene and DMF, and then, carrying out an N-alkylation reaction with 2-cyano-4'-bromo-methyl biphenyl, so as to obtain a compound III; subjecting the compound III and sodium azide to a reaction in DMF in the presence of zinc chloride, so as to obtain a compound II; and subjecting the compound II to a thio amidation reaction with a Lawesson's reagent, therebyobtaining the target product I. According to the method, the process is simple, the operation is simple and convenient, the raw materials are readily available, and the method is economical and efficient, so that the production cost of the Fimasartan is greatly reduced, and the industrial production is easy to achieve.
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(2018/05/16)

Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonists
The discovery, in vitro and in vivo studies of the highly potent AT1 antagonist 12a (BR-A-657, Fimasartan) are presented. A series of pyrimidin-4(3H)-one derivatives as losartan analogue were synthesized and evaluated for a novel class of AT1 receptor antagonists. Among them, 12a containing thioamido moiety displayed both high in vitro functional antagonism and binding affinity [IC50 = 0.42 and 0.13 nM, respectively] and inhibited strongly in vivo AngII-induced pressor response in pithed rats with an ED50 of 0.018 mg/kg. Moreover, in vivo evaluation in furosemide-treated rat and conscious renal hypertensive rat models and the pharmacokinetic study showed that 12a is a highly potent and orally active AT1 selective antagonist having stronger in vivo potency than losartan.
Kim, Tae Woo,Yoo, Byoung Wook,Lee, Joon Kwang,Kim, Ji Han,Lee, Kyung-Tae,Chi, Yong Ha,Lee, Jae Yeol
p. 1649 - 1654
(2012/04/04)

Pyrimidinone compounds, pharmaceutical compositions containing the compounds and the process for preparing the same
The present invention relates to a novel pyrimidinone compounds and the pharmaceutical acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, thereby, being useful in treating cardiovascular disease caused by binding angiotensin II to its receptor.
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(2008/06/13)