- Synthesis and Antifungal and Insecticidal Activities of Novel N -Phenylbenzamide Derivatives Bearing a Trifluoromethylpyrimidine Moiety
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Seventeen novel N-phenylbenzamide derivatives bearing a trifluoromethylpyrimidine moiety were synthesized via four-step reactions. Their antifungal and insecticidal properties were evaluated. Antifungal test results demonstrated that some of the synthesized compounds showed better in vitro bioactivities against Phomopsis sp., Botryosphaeria dothidea (B. dothidea), and Botrytis cinerea (B. cinerea) at 50 μg/mL than pyrimethanil. Unfortunately, the synthesized compounds revealed lower insecticidal activities against Spodoptera frugiperda (S. frugiperda) and Mythimna separata (M. separata) at 500 μg/mL than chlorantraniliprole.
- Yu, Xuetong,Lan, Wenjun,Chen, Meihang,Xu, Su,Luo, Xiaoxi,He, Shuhong,Chen, Haijiang,Fei, Qiang,Wu, Wenneng
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- Trifluoromethyl pyrimidine containing Ferulamide derivative and preparation and use thereof
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The invention discloses a trifluoromethyl pyrimidine containing Ferulamide derivative. The trifluoromethyl pyrimidine containing Ferulamide derivative is characterized by having a structural general formula represented by (I) shown in the description, wherein R1 is H, methyl, ethyl, n-propyl, isopropyl, n-butyl, phenyl, methylmercapto, ethylmercapto, fluoro-, chloro-, bromo-, trifluoromethyl and N,N-dimethylamine, R2 is monosubstituted, disubstituted and trisubstituted, and R2 is H, methyl, ethyl, methoxy, ethoxy, fluoro-, chloro-, bromo-, iodo-, trifluoromethyl, nitro- and hydroxyl. The trifluoromethyl pyrimidine containing Ferulamide derivative can resist major pathogenic bacteria, i.e., Phomopsis Sp. and Botryosphaeria dothidea of kiwi fruit soft rot.
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Paragraph 0020; 0024-0025; 0068; 0072-0073
(2019/08/20)
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- COMPOUNDS AS MODULATORS OF ROR GAMMA
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The present invention encompasses compounds of the formula (I)(I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
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Page/Page column 133
(2019/03/28)
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- Synthesis method of 6-trifluoromethyl-N-(2-trifluoromethylindole-5-yl)methyl-4-pyrimidinamine
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The invention discloses a synthesis method of 6-trifluoromethyl-N-(2-trifluoromethylindole-5-yl)methyl-4-pyrimidinamine, relates to a chemical synthesis method, and especially relates to a novel synthesis method of 6-trifluoromethyl-N-(2-trifluoromethylindole-5-yl)methyl-4-pyrimidinamine. According to the synthesis method, 6-trifluoromethyl-N-(2-trifluoromethylindole-5-yl)methyl-4-pyrimidinamine is obtained through Claisen condensation, cyclization, chlorination, and hydrocarbonylation reactions. Compared with the conventional methods, the cyclization is improved, materials can be continuously fed in chlorination and hydrocarbonylation steps, one-pot operation is realized, and the method is suitable for industrial production.
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Paragraph 0014; 0015; 0019
(2017/02/23)
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- AZAINDOLE COMPOUNDS AS MODULATORS OF RORC
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The present invention encompasses compounds of the formula (I), wherein the variables are defined herein which are suitable for the modulation of RORC and the treatment of diseases related to the modulation of RORC. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
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Page/Page column 66
(2015/02/25)
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- CYCLOPROPANECARBOXAMIDO-SUBSTITUTE AROMATIC COMPOUNDS AS ANTI-TUMOR AGENTS
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Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
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Paragraph 0393; 0394
(2015/07/22)
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- COMPOUNDS AS MODULATORS OF ROR GAMMA
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The present invention encompasses compounds of the formula (I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
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Page/Page column 144-145
(2015/11/09)
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- PYRIMIDINE COMPOUND AND ITS USE IN PEST CONTROL
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A pyrimidine compound represented by below formula (I) has excellent control activity against pests and is useful as an active ingredient of a pest controlling agent.
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Page/Page column 147
(2010/12/18)
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- QUINAZOLIN-4-ONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
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Page/Page column 37
(2008/06/13)
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- Metal-bearing and trifluoromethyl-substituted pyrimidines: Generation and functionalization
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5-Pyrimidyllithium species are fairly stable when the metal is flanked by two electron-withdrawing substituents such as trifluoromethyl and chlorine or bromine. Thus, the corresponding 5-carboxylic acids are produced in high yields from 4,5-dibromo-6-(trifluoromethyl)pyrimidine and 5-bromo-4-chloro-6- (trifluoromethyl)pyrimidine upon halogen/metal permutation accomplished with isopropylmagnesium chloride or butyllithium followed by carboxylation. Satisfactory or excellent yields of 5-carboxylic acids are equally obtained when 4-chloro-, 2,4-dichloro- and 2,4-dibromo-6-(trifluoromethyl)pyrimidine are deprotonated with lithium diisopropylamide before being allowed to react with dry ice. In contrast, consecutive treatment of 2-bromo-4-(trifluoromethyl) pyrimidine and 2-chloro-5-iodo-4-(trifluoromethyl)pyrimidine with butyllithium affords the expected carboxylic acids in only poor yields and not even trace amounts of acid were detected when 4-bromo-6-(trifluoromethyl)pyrimidine served as the substrate. The formation of bipyrimidines, emerging from either one of two competing mechanistic pathways, is a permanently menacing side reaction. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.
- Schlosser, Manfred,Lefebvre, Olivier,Ondi, Levente
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p. 1593 - 1598
(2007/10/03)
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- 3-AMINOCYCLOPENTANECARBOXAMIDES AS MODULATORS OF CHEMOKINE RECEPTORS
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The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
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Page/Page column 39-40
(2008/06/13)
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- BENZOYL-PIPERAZINE DERIVATIVES
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The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
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Page/Page column 26
(2008/06/13)
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- Herbicidal 5-substituted pyrimidine compounds and derivatives thereof
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Herbicidal 5-substituted pyrimidine compounds and derivatives thereof of the formula: STR1 Herbicidal compositions containing such 5-substituted pyrimidine compounds and derivatives thereof and methods of controlling undesirable vegetation using these compounds and derivatives are also disclosed. The compounds in which XR is hydroxyl are also useful as intermediates for producing the 5-substituted pyrimidine derivatives of the invention.
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