- Synthesis of benzotriazine and aryltriazene derivatives starting from 2-azidobenzonitrile derivatives
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3-Substituted 3,4-dihydro-4-imino-1,2,3-benzotriazine derivatives 7 were formed from 2-azidobenzonitriles 4 as starting materials on treatment with Grignard or lithium organic reagents. In some cases these procedures gave aryltriazenes 10 and 11 as products. All compounds were identified by NMR spectroscopy and the structures of three products, namely 7a, 10a and 11i, were corroborated by X-ray crystallography. The reactions of 2-azidobenzonitrile derivatives with Grignard reagents have been investigated. These reactions, depending on the type of Grignard reagent and the substituents on the 2-azidobenzonitrile derivatives, resulted in benzotriazines and triazenes. Copyright
- Nakhai, Azadeh,Stensland, Birgitta,Svensson, Per H.,Bergman, Jan
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experimental part
p. 6588 - 6599
(2011/02/26)
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- Discovery, Modeling, and Human Pharmacokinetics of N-(2-Acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl) -thiophene-2-carboxamide (TBC3711), a Second Generation, ETA Selective, and Orally Bioavailable Endothelin Antagonist
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Sitaxsentan (1) (Wu et al. J. Med. Chem. 1997, 40, 1690) is our first endothelin antagonist being evaluated in clinical trials. It has demonstrated biological effects in an acute hemodynamic study in CHF (Givertz et al. Circulation 2000, 101, 2922), an op
- Wu, Chengde,Decker, E. Radford,Blok, Natalie,Bui, Huong,You, Tony J.,Wang, Junmei,Bourgoyne, Andree R.,Knowles, Vippra,Berens, Kurt L.,Holland, George W.,Brock, Tommy A.,Dixon, Richard A. F.
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p. 1969 - 1986
(2007/10/03)
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- N-heteroaryl aryl-substituted thienyl-furyl-and pyrrolyl-sulfonamides and derviatives thereof that modulate the activity of endothelin
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Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit the activity of endothelin are also provided.
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