- Process for Preparation of Fimasartan and Intermediate for Preparing the Same
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The present invention relates to a simple and economically process for preparing fimasartan and its preparation intermediates. (by machine translation)
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- Method for preparing Fimasartan
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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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Paragraph 0049; 0050
(2019/01/16)
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- Preparation method of fimasartan potassium salt trihydrate
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The invention discloses a preparation method of fimasartan potassium salt trihydrate. The preparation method comprises the following steps: adding acyl halide into a solvent containing low alcohol toremove the triphenylmethyl group of a thioamide compound
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Paragraph 0038; 0039
(2018/04/02)
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- Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonists
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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
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p. 1649 - 1654
(2012/04/04)
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