- N-Alkylation of Imidazoles with Dialkyl and Alkylene Carbonates
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Abstract: The reactions of imidazoles with a series of dialkyl and alkylene carbonatesafforded the corresponding N-alkyl- andN-(hydroxyalkyl)imidazoles with highyields. The reactivity of dialkyl carbonates decreases in the series dimethyl> diethyl > dibutyl carbonate. Ethylene carbonate is a more efficientalkylating agent than trimethylene carbonate. The mechanisms of alkylation ofimidazole with dimethyl carbonate and ethylene carbonate were studied by DFTquantum chemical calculations at the B3LYP/6-311++G(d,p) level of theory.
- Gabov,Khamidullina,Puzyrev,Ezhikova,Kodess,Pestov
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p. 2079 - 2086
(2021/02/09)
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- QUINAZOLINE DERIVATIVE
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Provided are a quinazoline derivative, a pharmaceutical composition containing the same, a method for preparation of said derivative, and an application of same as an anti-cancer drug.
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Paragraph 0090
(2017/07/04)
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- FLAVIN DERIVATIVES
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The present invention relates novel flavin derivatives and other flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives. The invention also provides method of making novel flavin derivatives.
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Page/Page column 206-207
(2011/02/24)
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- FLAVIN DERIVATIVES
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The present invention relates novel flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives.
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Page/Page column 165-166
(2011/10/31)
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- AGENT FOR IMPROVING PERMEATION OF A DRUG INTO A NAIL AND AN EXTERNAL TREATING AGENT CONTAINING THE SAME
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The present invention herein provides a compound which promotes drug-permeation into nails. A penetrating promoter comprises, for instance, the following formulas. R1, R2 and R3 are alkyl groups having a carbon number of 1 to 15 and have OH groups at their ends.
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Page/Page column 5
(2010/04/23)
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- Hydantoin derivatives as non-peptidic inhibitors of Ras farnesyl transferase
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1,3,5,5-Tetrasubstituted 2,4-imidazolinedione (hydantoin) derivatives were evaluated as Ftase inhibitors. Potent Ftase inhibitors without thiol or peptide were obtained in three steps.
- Lee, Jinho,Kim, Jonghyun,Koh, Jong Sung,Chung, Hyun-Ho,Kim, Kyoung-Hee
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p. 1954 - 1956
(2007/10/03)
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- Synthesis of ω-carbamoyloxyalkylimidazolium salts for evaluation as protective agents against acetylcholinesterase intoxication by soman
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A series of N-methyl and N,N-dimethylcarbamoyloxyalkylimidazolium salts has been prepared. The carbamoyloxyalkyl groups are varied from methyl through propyl at the 1,2 or 4 positions of the imidazolium ring. The 2- and 4-substituted series show modest activity as inhibitors of acetylcholinesterase. Several of the compounds show prophylactic activity against soman toxicity but there is no correlation between AChE inhibitory activity and the prophylatic effect, suggesting that reversible carbamoylation is not the basis for the prophylactic effect.
- Sundberg, Richard J.,Van Nguyen, Phuoc
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p. 123 - 136
(2007/10/03)
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- Vitamin B12 derivative, preparation process thereof, and use thereof
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Vitamin B12 compounds, salts and pharmaceutical compositions containing said compounds represented by formula (I): STR1 wherein L, a ligand to the cobalt of the corrin ring, is selected from the group consisting of a cyano or adenosyl group, B is an imidazole group or a 5,6-dimethylbenzimidazole group, and R is a straight alkylene group having 1 to 8 carbon atoms, are disclosed. Methods for preparing compounds of Formula (I) as well as methods for using the compounds in in vitro assays, in cell growth studies and in in vivo studies using transplanted murine tumor cells are disclosed.
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- Preparation of 1-substituted imidazoles
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A process for the preparation of 1-substituted imidazoles by reacting an α-dicarbonyl compound with ammonia, an aldehyde and a primary amine in an aqueous medium, in a single stage, at 20°-150° C.
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