133690-92-3Relevant academic research and scientific papers
New technology for preparing azilsartan
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Paragraph 0020; 0021, (2017/11/29)
The invention relates to a preparation method for azilsartan. The method is characterized by comprising the following steps: enabling 2-fluorine-3-bromine nitrobenzene to react with a midbody 3 prepared from suzuki reaction, replacing 2 fluorines and then reducing by nitro group; reacting with tetraethyl orthocarbonate, closing the ring and forming a benzimidazole ring; reacting with hydroxylamine hydrochloride and compounding a phenyl substituted oxadiazole ring under the effect of CDI; forming formic acid with carbon dioxide under the catalysis of n-butyllithium, thereby acquiring the product. The preparation method has the advantages of easily acquired raw materials, simple process, high overall yield, few side products, simplicity in post-processing and suitability for industrial production.
Sequential one-pot access to molecular diversity through aniline aqueous borylation
Erb, William,Albini, Mathieu,Rouden, Jacques,Blanchet, Jrme
, p. 10568 - 10580 (2015/01/08)
On the basis of our recently reported aniline aqueous borylation, molecular diversity was achieved in a one-pot process by combining other reactions such as esterification, Suzuki-Miyaura coupling, hydrogenolysis, or Petasis borono-Mannich.
Anti-Inflammation Compounds
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Paragraph 0118; 0128, (2014/06/23)
The present invention refers to: a compound having the general formula (I), wherein n is 0, 1, 2 or; m is 0, 1, 2 or 3; o is 0, 1, 2 or 3; W, X, Y and Z are independently selected from CH, N or N-oxide; A is NR4, C═O, C═S, OP(O)(O), P═O, CH2, or a heteroarly selected from the group consisting of (a), (b), (c), (d), (e), (f), (g); V is C═O, O, S, CH2, or NR5; as well as its use in treating inflammatory diseases such as asthma, COPD, inflammation post infection, arthritis, atherosclerosis, pain and dermatitis.
Improved methods for the synthesis of irbesartan, an antihypertensive active pharmaceutical ingredient
Rao, Korrapati V. V. Prasada,Dandala, Ramesh,Handa, Vijay K.,Rao, Inti V. Subramanyeswara,Rani, Ananta,Naidu, Andra
, p. 2897 - 2905 (2008/02/13)
New methods for the preparation of irbesartan 1 have been described. The dehydration and tetrazole formation in one step from substituted cyclopentane derivative 7 with tributyltin chloride and sodium azide is described. Selective hydrolysis of nitrile 3 with HCl has also been described in the preparation of N-acylaminocyclopentane-2-carboxylic acid 4, which is the key intermediate for the preparation of irbesartan. The impurity profiling of irbesartan has also been discussed. Copyright Taylor & Francis Group, LLC.
AN IMPROVED PROCESS FOR THE PREPARATION OF IRBESARTAN
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Page/Page column 14-15, (2008/06/13)
The present invention relates to an improved process for the preparation of 2-n-butyl-3-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]-1,3-diazaspiro[4.4]non-1-en-4-one (Irbesartan)
SUBSTITUTED 1,2,4-TRIAZOLES BEARING ACIDIC FUNCTIONAL GROUPS AS ANGIOTENSIN II ANTAGONISTS
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, (2008/06/13)
Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists. STR1
SUBSTITUTED TRIAZOLES AS ANGIOTENSIN II ANTAGONISTS
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, (2008/06/13)
Novel substituted triazoles of the formula (I), which are useful as angiotensin II antagonists, are disclosed. STR1
Substituted n-biphenylyl lactams
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, (2008/06/13)
This invention relates to novel N-biphenylyl lactam compounds having a substituted methylidene or methyl moiety adjacent to the lactam nitrogen, and pharmaceutically acceptable salts thereof.The compounds are angiotensin II receptor antagonists, and are u
Synthesis and Structure-Activity Relationships of Nonpeptide, Potent Triazolone-Based Angiotensin II Receptor Antagonists
Huang, Horng-Chih,Reitz, David B.,Chamberlain, Timothy S.,Olins, Gillian M.,Corpus. Valerie M.,et al.
, p. 2172 - 2181 (2007/10/02)
2,5-Dibutyl-2,4-dihydro-4--4'-yl>methyl>-3H-1,2,4-triazol-3-one, SC-51316, was synthesized as a potent and orally active angiotensin II (AII) receptor antagonist with a long duration of action.To explore the lipophilic pocket in the AII receptor interacting with the substituent at the 2-position of triazolone-based antagonists, a series of compounds were prepared and evaluated for receptor binding affinity and antagonism of AII-contracted rabbitaortic rings.It has been found that the pocket is very spacious and can accommodate different sizes of lipophilic groups and various functionalities.Acidic groups generally result in a slight decrease in binding affinity.Branched chains are unfavorable.The freedom of rotation around C2-C3 in the flexible side chain is crucial for good binding.The 2-phenylethyl-substituted triazolone analogue exhibits the highest in vitro potency among all compounds that have been synthesized.
