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A mild and effective method for asymmetric synthesis of C2-quaternary indolin-3-ones directly from 2-arylindoles by combining visible light photocatalysis and organocatalysis is described. In this reaction, 2-substituted indoles undergo photocatalyzed oxidative dearomatization, followed by an organocatalyzed asymmetric Mannich reaction with ketones or aldehydes. Products with opposite configurations are easily obtained in satisfactory yields with excellent enantio- A nd diastereoselectivity by employing readily available l- A nd d-proline as chiral organocatalysts.

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A trifluoroacetic acid promoted step-economical one-pot approach to the synthesis of furo-fused quinoxalines/pyrazines by the reaction of 2,3-dichloroquinoxalines/pyrazines with alkynes is described. The reaction involves a selective in-situ Sonogashira coupling step and a hydroxylation followed by a metal-free 5-endo-dig cyclization. Preliminary experiments show that trifluoroacetic acid acts as a source of oxygen for the oxyarylation step, and isotopic labeling studies support the proposal that the mechanistic pathway involves activation of the alkyne by the acidic medium. Various kinds of substituents are tolerated, which should prove valuable for structural and biological investigations.

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Some new quinoxaline-6-sulfonamide and phthalazine-6-sulfonamide derivatives were synthesized. The majority of the prepared compounds showed antibacterial activity.

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2-{4-[(7-Chloro-2-quinoxalinyl)oxy]phenoxy}propionic acid (XK469) is among the most highly and broadly active antitumor agents to have been evaluated in our laboratories and is currently scheduled to enter clinical trials in 2001. The mechanism or mechanisms of action of XK469 remain to be elaborated. Accordingly, an effort was initiated to establish a pharmacophore hypothesis to delineate the requirements of the active site, via a comprehensive program of synthesis of analogues of XK469 and evaluation of the effects of structural modification(s) on solid tumor activity. The strategy formulated chose to dissect the two-dimensional parent structure into three regions – I, ring A of quinoxaline; II, the hydroquinone connector linkage; and III, the lactic acid moiety – to determine the resultant in vitro and in vivo effects of chemical alterations in each region. Neither the A-ring unsubstituted nor the B-ring 3-chloro-regioisomer of XK469 showed antitumor activity. The modulating antitumor effect(s) of substituents of differing electronegativities, located at the several sites comprising the A-ring of region I, were next ascertained. Thus, a halogen substituent, located at the 7-position of a 2-{4-[(2-quinoxalinyl)oxy]phenoxy}propionic acid, generated the most highly and broadly active antitumor agents. A methyl, methoxy, or an azido substituent at this site generated a much less active structure, whereas 5-, 6-, 8-chloro-, 6-, 7-nitro, and 7-amino derivatives all proved to be essentially inactive. When the connector linkage (region II) of 1 was changed from that of a hydroquinone to either a resorcinol or a catechol derivative, all antitumor activity was lost. Of the carboxylic acid derivatives of XK469 (region III), i.e., CONH2, CONHCH3, CON(CH3)2, CONHOH, CONHNH2, CN, or CN4H (tetrazole), only the monomethyl- and N,N-dimethylamides proved to be active.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N1622 | ChemSpider

 

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Compounds and pharmaceutically acceptable salts thereof of Formula I are disclosed. Certain compounds and salts of Formula I are active as CMA modulators. The disclosure provides pharmaceutical compositions containing a compound of Formula I.

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The synthesis, single-crystal X-ray structure and magnetic properties of [Cu3L2Cl2(DMF)4]n (1), where L2- is the 2,3-dioxyquinoxalinate(-2) ligand, are reported. The complex was prepared by the reaction of CuCl2 and 1,4-dihydro-2,3-quinoxalinedione (H2L?) under basic conditions using either solvothermal or normal laboratory techniques. Compound 1 is a 3D coordination polymer with an (82.10)-a, lig (LiGe) topology, containing the ligand in a novel 3.1111 (Harris notation) coordination mode. Variable-temperature and variable-field magnetic studies reveal that the ligand L2- propagates weak antiferromagnetic exchange interactions through its “quinoxaline” part. IR data are discussed in terms of the structural features of 1 and the coordination mode of L2-.

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Formula: C10H8N2O, New Advances in Chemical Research in 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 25594-62-1, Name is 2-Acetylquinoxaline, molecular formula is C10H8N2O. In a article,once mentioned of 25594-62-1

A nickel-catalyzed electrochemical methodology for the Minisci acylation of aromatic electron-deficient heterocycles with alpha-keto acids has been developed. The reaction is performed in an undivided cell under constant current conditions, featuring broad scope of substrates and avoiding the conventional utilization of silver-based catalysts in conjunction with excess amount of oxidants. Cyclic voltammetric analysis disclosed that a ligand-to-metal electron transfer process may be involved in the generation of the key acyl radicals.

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A herbicidal composition which comprises an adjuvant and an active ingredient of heterocyclic ether type phenoxy fatty acid derivative having the formula STR1 wherein A represents –CH– or –N–; X represents a halogen atom; n is 0, 1 or 2; R1 represents a hydrogen atom; a lower alkyl group; R2 represents –OH; –O-alkyl group; –OM group (M is an inorganic or organic salt moiety); STR2 –O-lower alkenyl group; –O-benzyl group; –O-lower alkylalkoxy group; –O-phenyl; –O-cyclohexyl, –O-halogenoalkyl, –O-lower alkynyl and –O-cyanoalkyl; R3 and R4 respectively represent a hydrogen atom or a lower alkyl group.

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A facile and efficient protocol for palladium-catalyzed Miyaura borylation reaction of chloropyrazines with B2pin2has been developed. A certain range of difficult-to-access pyrazine boronic esters can be easily prepared from the corresponding chloropyrazines in moderate to good yields.

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A series of phthalazinyl- and quinoxalinylguanidines has been synthesized and evaluated for potential antihypertensive activity.Unsubstituted guanidines were prepared by treating the appropriate intermediate chloro compounds with guanidine free base.Substituted guanidines were prepared by treating the cyanamides 9 and 16 with the appropriate amine; with hydrazines, cyanamide 9 gave the triazoles 14 and 15.Moderate falls in blood pressure were observed with compounds 10, 11, 14, and 15.The triazole 15 caused a 25percent fall in heart rate.Some of the compounds (10, 11, 13, and 18) displayed weak alpha-adrenoceptor antagonist properties in vitro, and this activity was confirmed in the pithed rat (in vivo).

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