150869-58-2Relevant academic research and scientific papers
Process for the preparation of tetrazoles
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, (2008/06/13)
The present invention relates to a process for the preparation of 5-aryl tetrazoles of the formula: STR1 or a salt thereof comprising reacting an aryl nitrile with a trisubstituted silyl azide and a disubstituted tin oxide.
2-(Alkylamino)nicotinic Acid and Analogs. Potent Angiotensin II Antagonists
Winn, Martin,De, Biswanath,Zydowsky, Thomas M.,Altenbach, Robert J.,Basha, Fatima Z.,et al.
, p. 2676 - 2688 (2007/10/02)
A series of pyridines and other six-membered ring heterocycles connected to a biphenyltetrazole with a-CH2-NR'-link (1) were discovered to be potent angiotensin II antagonists.In the pyrimidine carboxylic acid series (W = CR, X = N, Y = CH, Z = COOH), compounds with an alkyl group (R') on the exocyclic nitrogen were much more potent than compounds with an alkyl group (R) on the heterocyclic ring.The corresponding pyridine, pyridazine, pyrazine, and 1,2,4-triazine carboxylic acids also showed potent in vitro angiotensin II antagonism.The pyridine (W, X, Y = CH, Z = COOH, R' = n-C3H7) demonstrated potent in vitro activity (pA2 = 10.10, rabbit aorta, and Ki = 0.61 nM, receptor binding in rat liver) as well as exceptional oral antihypertensive activity and bioavailability.Any nonacidic replacement for the carboxylic acid was detrimental for activity.
An efficient synthesis of an angiotensin II antagonist (A-81988)
Kerdesky,Haight,Narayanan,Nordeen,Scarpetti,Seif,Wittenberger,Morton
, p. 2027 - 2039 (2007/10/02)
A new and efficient synthesis of A-81988, an angiotensin II antagonist, is described. The preparation utilizes a novel method for tetrazole formation from nitriles requiring trimethylsilyl azide and a catalytic amount of dialkyltin oxide.
1,3-oxazolyl substituted biphenyl
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, (2008/06/13)
The present invention relates to a process for the preparation of a compound of the formula: STR1 wherein R1 is selected from the group consisting of hydrogen, loweralkyl, loweralkoxy-substituted loweralkyl, lower alkenyl, lower alkynyl, cycloalkyl and cycloalkylalkyl; R2 is selected from the group consisting of hydrogen, loweralkyl, loweralkoxy-substituted loweralkyl, halogen and loweralkoxy; R3 is selected from hydrogen, loweralkyl, and halogen; R* and R** are independently selected from loweralkyl and P1 is hydrogen or an nitrogen-protecting group; or an acid addition salt thereof.
