- Preparation of Imidazole Derivatives via Bisfunctionalization of Alkynes Catalyzed by Ruthenium Carbonyl
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A one-step, oxidative bisfunctionalization of alkynes to generate cis -enediol diacetates catalyzed by ruthenium carbonyl (triruthenium dodecacarbonyl) is presented. The reaction was performed using the alkyne, (diacetoxyiodo)benzene, Ru 3 (CO) 12 as the catalyst, and toluene as the solvent at 100 °C to give the cis -enediol diacetates in up to 82percent yields. This method overcomes the shortcomings of existing methods, such as tedious reaction steps, substrate limitations, and the use of toxic reagents. Furthermore, the reaction of module cis -enediol diacetates with ammonium carbonate [(NH 4) 2 CO 3 ] in an alcohol solvent gave imidazole derivatives in 37-84percent yields, thus providing a simple and mild new method for the synthesis of imidazole compounds.
- Chen, Yue-Peng,Gu, Ling-Hui,He, Ling,Luo, Yang,Ruan, Yi-Tong,Yang, Ze
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p. 3520 - 3528
(2019/09/07)
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- SPIROCYCLIC COMPOUNDS
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Disclosed herein are spirocyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.
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Paragraph 0289
(2017/07/31)
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- IDO inhibitors
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Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R1, R4, and R5 are defined herein. Such compounds and compositions are useful for mod
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Page/Page column 204-205
(2015/11/27)
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- Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2- ones as potent and selective mTOR kinase inhibitors
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We report here the discovery of a novel series of selective mTOR kinase inhibitors. A series of imidazo[4,5-b]pyrazin-2-ones, represented by screening hit 1, was developed into lead compounds with excellent mTOR potency and exquisite kinase selectivity. Potent compounds from this series show >1000-fold selectivity over the related PI3Kα lipid kinase. Further, compounds such as 2 achieve mTOR pathway inhibition, blocking both mTORC1 and mTORC2 signaling, in PC3 cancer cells as measured by inhibition of pS6 and pAkt (S473).
- Mortensen, Deborah S.,Perrin-Ninkovic, Sophie M.,Harris, Roy,Lee, Branden G.S.,Shevlin, Graziella,Hickman, Matt,Khambatta, Gody,Bisonette, Rene R.,Fultz, Kimberly E.,Sankar, Sabita
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p. 6793 - 6799
(2012/01/03)
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- IMIDAZOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH AND AS FAAH IMAGING AGENTS
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The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds
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Page/Page column 32
(2010/09/18)
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- HETEROARYL COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Provided herein are Heteroaryl Compounds having the following structure: (I) wherein R1, R2, L, X, Y, Z, Q, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
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Page/Page column 197
(2008/12/05)
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- 4-RING IMIDAZOLE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
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Imidazole compounds of Formula (I): (where A, B, R11, R12, W, X. Y and Z are as defined herein) wherein the imidazole is substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl a
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