1361024-52-3

Upstream product

• 503155-65-5 C₁₃H₂₀N₂O₃ 
• 503155-66-6 C₄₆H₄₄N₆O₃ 
• 1361024-33-0 C₄₄H₄₀N₆O₃ 
• 503155-67-7 2-n-butyl-5-dimethylaminocarbonylmethyl-6-methyl-3-[[2'-(N-triphenylmethyltetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidin-4(3H)-one 
• 110-59-8 pentanonitrile 
• 1315478-16-0 2-(2-n-butyl-4-hydroxy-6-methyl-pyrimidin-5-yl)acetic acid 
• 1315478-13-7 (2-(2-n-butyl-4-hydroxy-6-methyl-pyrimidin-5-yl)-N,N-dimethylacetamide) 
• 124750-51-2 N-(triephenylmethyl)-5-<4'-(bromomethyl)-biphenyl-2-yl>tetrazole 

Downstream Products

• 247257-48-3 Fimasartan 

Relevant academic research and scientific papers

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)

Preparation method of fimasartan potassium salt trihydrate

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

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.

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.