- Carbonylative Acetylation of Heterocycles
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Herein, a new procedure for the carbonylative acetylation of heterocycles has been developed. In this process, organic peroxide acts as the methyl source. Various heterocycles were transformed into the corresponding methyl heterocyclic ketones in moderate to good yields.
- Zhang, Youcan,Yin, Zhiping,Wu, Xiao-Feng
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supporting information
p. 213 - 216
(2020/01/22)
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- Direct C-2 acylation of thiazoles with aldehydes via metal- and solvent-free c-h activation in the presence of tert-butyl hydroperoxide
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A novel and efficient methodology for the synthesis of heteroaryl ketones by C-H activation of aldehydes and thiazoles is developed. The reaction occurs smoothly, under metal-, acid- and solvent-free conditions using tert-butyl hydroperoxide as the oxidant under an air atmosphere, to afford a wide range of heteroaryl ketones in moderate to good yields. The sp2 C-H bonds in the aldehyde and thiazole undergo direct oxidative cross-coupling, resulting in C-2 acylation of the azole. Georg Thieme Verlag Stuttgart · New York.
- Khemnar, Ashok B.,Bhanage, Bhalchandra M.
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supporting information
p. 110 - 114
(2014/01/06)
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- New 1,2,4-triazine derivatives and biological applications thereof
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The invention relates to new 1,2,4-triazine derivatives of formula (I): wherein A, B, R2 and Y are defined in the application, their preparation and intermediates, their use as drugs and pharmaceutical compositions and associations containing them. The compounds of formula (I) are capable of inhibiting bacterial heptose synthesis.
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Page/Page column 41
(2010/01/29)
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- QUINOLINE DERIVATIVES AND QUINAZOLINE DERIVATIVES INHIBITING AUTOPHOSPHORYLATION OF MACROPHAGE COLONY STIMULATING FACTOR RECEPTOR
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An objective of the present invention is to provide compounds which have inhibitory activity against autophosphorylation of macrophage colony-stimulating factor receptors. The compounds of the present invention are represented by formula (I) and salt and solvate thereof: wherein X represents CH or N; Z represents O or S; R1, R2, and R3 represent H, optionally substituted alkoxy or the like; R4 represents H; R5, R6, R7, and R8 represent H, halogen, alkyl, alkoxy, trifluoromethyl or the like; R9 and R10 represent H, alkyl or the like; and any one of R11 and R12 represents H with the other representing alkyl and R13 represents an optionally substituted carbocyclic or heterocyclic ring or the like, or R11 represents H and R12 and R13 combine together to form a bicyclic carbocyclic ring.
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Page/Page column 25
(2008/06/13)
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- THIAZOLES USEFUL AS INHIBITORS OF PROTEIN KINASES
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The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
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