- New synthetic approaches towards analogues of bedaquiline
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Multi-drug resistant tuberculosis (MDR-TB) is of growing global concern and threatens to undermine increasing efforts to control the worldwide spread of tuberculosis (TB). Bedaquiline has recently emerged as a new drug developed to specifically treat MDR-
- Priebbenow, Daniel L.,Barbaro, Lisa,Baell, Jonathan B.
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p. 9622 - 9628
(2016/10/25)
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- MATERIAL FOR ORGANIC ELECTROLUMINESCENT ELEMENTS, ORGANIC ELECTROLUMINESCENT ELEMENT USING SAME, AND ELECTRONIC DEVICE
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A material for an organic electroluminescence device including a compound represented by any of the formulas (1) to (3):
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Paragraph 0309; 0312; 0313
(2016/10/17)
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- Synthesis and in vitro antiproliferative activities of quinoline derivatives
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The synthesis of new di- and trimeric quinoline derivatives is described as well as their in vitro antiproliferative activities toward a human fibroblast primary culture and two human solid cancer cell lines (MCF-7 and PA 1).
- Broch, Sidonie,Aboab, Bettina,Anizon, Fabrice,Moreau, Pascale
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experimental part
p. 1657 - 1662
(2010/05/18)
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- Efficient syntheses of KDR kinase inhibitors using a Pd-catalyzed tandem C-N/suzuki coupling as the key step
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(Chemical Equation Presented) A family of four potent KDR kinase inhibitors containing an indol-2-yl quinolin-2-one structure was utilizing a Pd-catalyzed tandem C-N and C-C coupling sequence.
- Fang, Yuan-Qing,Karisch, Robert,Lautens, Mark
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p. 1341 - 1346
(2007/10/03)
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- 2-SUBSTITUTED INDOLES, THEIR PRECURSORS AND NOVEL PROCESSES FOR THE PREPARATION THEREOF
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Disclosed are processes for the preparation of 2-substituted indole compounds wherein the 2-substituent comprises an R4 group, wherein R4 is selected from the group consisting of monocyclic aromatic, polycyclic aromatic, monocyclic heteroaromatic, polycyclic heteroaromatic, 1° alkyl, and alkenyl, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents, and wherein R4 is bonded to the 2-position of the indole ring via a C-C bond; the process comprising reacting an ortho-gem-dihalovinylaniline compound of the formula (I): wherein Halo comprises Br, Cl, or I; each of the one or more R1 is independently selected from the group consisting of H, fluoro, lower alkyl, lower alkenyl, lower alkoxy, aryloxy, lower haloalkyl, lower alkenyl, -C(O)O-lower alkyl, monocyclic or polycyclic aryl or heteroaryl moiety, or R1 is an alkenyl group bonded so to as to form a 4- to 20-membered fused monocycle or polycyclic ring with the indole ring; all of which are optionally substituted with one or more suitable substituents at one or more substitutable positions; R2 comprises H, alkyl, cycloalkyl, aryl, heteroaryl, aryl-loweralkyl-, or heteroaryl-loweralkyl-, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents; R3 comprises H, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycle, aryl-(C1-6)alkyl-, or heteroaryl-loweralkyl-, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents; with an organoboron reagent selected from the group consisting of a boronic ester of R4, a boronic acid of R4, a boronic acid anhydride of R4, a trialkylborane of R4 and a 9-BBN derivative of R4; in the presence of a base, a palladium metal pre-catalyst and a ligand under reaction conditions effective to form the 2-substituted indole compound. Also disclosed are processes for the preparation of ortho-gem-dihalovinylaniline compounds. Novel compounds prepared by the processes and novel uses of the compounds are likewise disclosed.
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Page/Page column 73; 131-132
(2010/11/08)
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