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Chlorination with equimolar POCl3 can be efficiently achieved not only for hydroxypyrimidines, but also for many other substrates such as 2-hydroxy-pyridines,-quinoxalines, or even-amides. The procedure is solvent-free and involves heating in a sealed reactor at high temperatures using one equivalent of pyridine as base. It is suitable for large scale (multigram) batch preparations.

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Vilsmeier-Haack reaction, using a specific combination of phosphorus oxychloride and dimethylformamide, on 3-arylisoxazol-5(4H)ones 1 resulted in 2,4-dichloroquinoline-3-carbaldehydes 6 as the major products along with other minor products, through a novel rearrangement. Oxidation of 6 with alkaline potassium permanganate gave 2,4-dichloroquinoline-3-carboxylic acids 7. Decarboxylation of 6 and decarboxylation of 7 using aqueous sodium hydroxide yielded 2,4-dichloroquinolines 8. All the compounds were characterised by elemental and spectral analysis.

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Provided is compound of formula (I) where: X and Y may be identical or different and represent O, NH, or S; R 1, R 2, R 3, R 4, R 5, R 6, R 7, R 8, R 9, and R 10 may be identical or different and represent H, halogen, CN, NO 2, (C 1-4)alkyl, (C 1-4)haloalkyl, (C 2-4)alkenyl, OH, O(C 1-4)alkyl, O(C 1-4)haloalkyl, N(R A)R B, C(O)N(R A)R B, C(O)R A, CO 2R A, CHO, C 2-4alkenyl substituted with CN, C 2-4alkenyl substituted with COOH, C 2-4alkenyl substituted with CHO, or C 2-4alkenyl substituted with OH; R A and R B may be identical or different and represent H, (C 1-4)alkyl, (C 1-4)haloalkyl, or (C 2-4)alkenyl; A 1, A 2, A 3, and A 4 may be identical or different and represent CH or N with the proviso that A 1 and A 2 cannot be N and that R 5 and R 10 are absent when A 3 and A 4 are N; or a pharmaceutically acceptable salt thereof, stereoisomer thereof, or mixture comprising stereoisomers thereof.

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Sonochemical dehalogenation of 2,4-dichloroquinoline is very facile.However, with 5,7-dimethoxy-2,4-dichloroquinoline the reaction proceeds stepwise to provide the title dimethoxyquinolines which cannot be prepared via the Skraup reaction.The 13C NMR chemical shift assignments for 5,8-dimethoxyquinoline are presented.These were made by utilising the coupling connectivities from the bridgehead carbons in the 2D COLOC spectrum. – Keywords.Sonochemistry; Quinolines; 13C NMR Spectroscopy; 2D COLOC spectrum.

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Five new structural analogues of substituted-1H-quinolinones (19, 20, 23, 24, and 26) have been synthesized and evaluated for Staphylococcus aureus methionyl-tRNA synthetase enzyme inhibitory activity. These compounds were also tested against pathogens of six S. aureus, two Enterococcus faecalis, and one Enterococcus faecium. Among all the synthesized quinolinones, compound 20 displayed significant inhibitory activities in the strains of E. faecalis and E. faecium.

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This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.

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Methods employing and compositions comprising, for the control of plant-pathogenic organisms, specified s-triazolo(4,3-a)quinoline compounds, some of which are claimed as novel compounds.

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The present invention relates to 4-benzylaminoquinolines of the formula (I) or physiologically tolerated salts thereof. The invention relates to pharmaceutical compositions comprising such quinolines, and the use of such quinolines for therapeutic purposes. The quinolines are GIyTI inhibitors

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The present invention relates to compounds of formula I that function as inhibitors of BCL6(B- cell lymphoma 6) activity: Formula I wherein X1, X2, X3, R1, R2, R3, R4 and R5 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer,as well as other diseases or conditions in which BCL6 activity is implicated.

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This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein which exhibit strong inhibition effects on various cancer cell lines. The compounds disclosed herein are useful for the treatment of proliferative diseases, including neoplastic diseases such as cancer and non- neoplastic disorders such as rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient and optionally one or more additional therapeutically active agents, including anticancer agents. This application also discloses methods for treating a proliferative disease, including neoplastic diseases such as cancer and non- neoplastic disorders such as rheumatoid arthritis.

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