- Imidazole derivatives having an inhibitory activity for farnesyl transferase and process for preparation thereof
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The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1); and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.
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- A study of the Friedel-Crafts acylation of 1-benzenesulfonyl-1H-pyrrole in the preparation of 3-aroylpyrroles
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In this work, we studied the aluminum chloride catalyzed reaction of 1- benzenesulfonyl-1H-pyrrole with a series of eleven aroyl chlorides. The products formed were not isolated, but hydrolyzed to the target 3- aroylpyrroles in overall yields, usually, higher than 50%. However, in the CaSeS with the π electron rich 1-phenyl-1H-pyrrole-3-carbonyl chloride and 1-methyl-1H-indole-3-carbonyl chloride significant C-2 substitution occured, resulting in the isolation of the corresponding 1-benzenesulfonyl-2- aroylpyrroles as the predominant or the sole products. The desired C-3 isomers were synthesized starting with 1-triisopropylsilanyl-1H-pyrrole.
- Nicolaou, Ioannis,Demopoulos, Vassilis J.
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p. 1345 - 1348
(2007/10/03)
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- The regioselective photoinduced aroylation at the 3-position of pyrrole derivatives
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Irradiation of arenecarbothioamide with pyrrole or indole derivatives gave regioselectively 3-aroylpyrrole or -indole derivatives, respectively.
- Oda, Kazuaki,Hiratsuka, Rin,Machida, Minoru
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p. 463 - 470
(2007/10/03)
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- 1-Alkyl-3-(l-naphthoyl)pyrroles: A New Class of Cannabinoid
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The design and synthesis of a series of 1-alkyl-3-(1-naphthoyl)pyrroles is described. Molecular modeling studies were employed to aid in the design of these compounds. During the course of the synthesis the Friedel-Crafts reactions of N-aryl sulfonyl pyrroles were reinvestigated. The title compounds (4) were subjected to pharmacological evaluation and the data obtained have enabled these pyrroles to be classified as cannabinoids.
- Lainton, Julia A. H.,Huffman, John W.,Martin, Billy R.,Compton, David R.
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p. 1401 - 1404
(2007/10/02)
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