133690-92-3Relevant articles and documents
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.
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.
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.
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.