143945-72-6Relevant articles and documents
INTERMEDIATE COMPOUNDS FOR THE PREPARATION OF ANGIOTENSIN II RECEPTOR ANTAGONISTS
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Page/Page column 11, (2008/12/05)
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5-aryleheteroarylalkyl-1,3,5-trisubstituted-1,2,4-triazole compounds for treatment of circulatory disorders
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, (2008/06/13)
A class of 5-arylheteroarylalkyl-1,3,5-trisubstituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders such as hypertension. Compounds of particular interest are angiotensin II antagonists of the formula wherein A is selected from wherein m is one; wherein R1 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neo-pentyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl, 1,1-dimethoxypropyl, 1,1-dimethoxypentyl, halo, difluoromethyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluoro-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and butylthio; wherein each of R3, R4, R6 through R11 is hydrido and R5 is selected from COOH, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, wherein each of R42 and R43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl.
A novel and expeditious route to A-81988: An angiotensin II receptor antagonist
Kerdesky,Sowin
, p. 1007 - 1013 (2007/10/03)
A novel and efficient synthesis of A-81988, an angiotensin II receptor antagonist, is described. The key step utilizes a palladium-catalyzed biaryl coupling between a phenylboronic acid derivative and N-trityl-5-(2-bromophenyl)tetrazole.