- THIOPHENE DERIVATIVE
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The present invention provides a compound represented by the formula (I) or its salt, solvate, or physiologically functional derivative; and a pharmaceutical composition which is useful for treatment or prevention of conditions or disorders having sensitivity to selective androgen receptor modulation, the composition comprising the above-described compound; among others:
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Page/Page column 30-31
(2012/03/26)
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- Efficient synthesis of heterocyclic compounds using ethenetricarboxylic acid diesters
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Ethenetricarboxylic acid diester 1a is a useful compound bearing two reactive sites, a CO2H group and a Michael acceptor. Reactions of 1a and reagents with oxygen and nitrogen nucleophilic moieties have been examined. The reaction of 1a with 2-
- Yamazaki, Shoko,Iwata, Yuko,Fukushima, Yugo
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supporting information; experimental part
p. 655 - 659
(2009/06/20)
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- NEW BRADYKININ B1 ANTAGONISTS
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The invention relates to compounds of formula (I), wherein R1 to R5 and X1 to X4, n and m have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The
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Page/Page column 34; 45-46
(2008/12/08)
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- Carbamoylimidazolium and thiocarbamoylimidazolium salts: Novel reagents for the synthesis of ureas, thioureas, carbamates, thiocarbamates and amides
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Carbamoylimidazolium salts act as efficient N,N-disubstituted carbamoylating reagents. These salts are readily prepared by the sequential treatment of secondary amines with N,N′-carbonyldiimidazole (CDI) and iodomethane. The carbamoylimidazolium salts are more efficient carbamoyl transfer reagents than the intermediate carbamoylimidazoles, as a result of the 'imidazolium' effect. Kinetic studies on the base promoted hydrolysis of both carbamoylimidazoles and carbamoylimidazolium salts reveal over a hundred-fold rate acceleration. The salts react with amines, thiols, phenols/alcohols, and carboxylic acids in high yields, without the need for subsequent chromatographic purification of the products, producing ureas, thiocarbamates, carbamates, and amides, respectively. Analogous thiocarbamoylimidazolium salts were also synthesized from secondary amines and N,N′-thiocarbonyldiimidazole (TCDI), followed by methylation with iodomethane.
- Grzyb, Justyna A.,Shen, Ming,Yoshina-Ishii, Chiaki,Chi,Brown, R. Stanley,Batey, Robert A.
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p. 7153 - 7175
(2007/10/03)
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- Carbamoylimidazolium salts as diversification reagents: An application to the synthesis of tertiary amides from carboxylic acids
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An efficient method for the preparation of tertiary amides from carbamoylimidazolium salts and carboxylic acids is described. The transformation occurs at room temperature and under relatively mild conditions. The carbamoylimidazolium salts are obtained from the reaction of secondary amines with N,N′-carbonyldiimidazole, followed by methylation with methyl iodide. The utility of this reaction was demonstrated in the formation of Weinreb amides and in a short synthesis of fused bicyclic amides. The introduction of this reaction now permits carbamoylimidazolium salts to be utilized in the formation of tertiary amides, ureas, carbamates and thiocarbamates under a single set of conditions.
- Grzyb, Justyna A.,Batey, Robert A.
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p. 7485 - 7488
(2007/10/03)
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