- Synthesis and biological activity of novel 2-methyl-4-trifluoromethyl-thiazole-5-carboxamide derivatives
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Nine novel 2-methyl-4-trifluoromethylthiazole-5-carboxamide derivatives were designed and synthesized utilizing ethyl 4,4,4-trifluoroacetoacetate as a starting material. Subsequently, the biological activity of the compounds was evaluated in the greenhouse. Results indicated that all of the compounds have some fungicidal and insecticidal activity but no herbicidal activity. Compound 1 has fungicidal activity with 90% control of tomato late blight at 375 g ai/ha, while two compounds 2F and 2H show insecticidal activity with 80 and 100% control, respectively, against potato leafhopper at 600 g ai/ha.
- Liu, Chang-Ling,Li, Zheng-Ming,Zhong, Bin
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- Synthesis and Insecticidal Activity of Novel Thiazole Acrylonitrile Derivatives
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A series of novel thiazole acrylonitrile derivatives was designed and synthesized utilizing NC-510 as a precursor. Their structures were characterized by NMR spectrometry, MS, and elemental analysis. The results of bioassay indicated that some of these ti
- Cao, Shengwen,Liu, Aiping,Liu, Weidong,Liu, Xingping,Ren, Yeguo,Pei, Hui,Huang, Lu,Zheng, Xi,Huang, Mingzhi,Wu, Daoxin
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p. 3395 - 3402
(2017/11/21)
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- 2-methyl-4-(trifluoromethyl) thiazol-5-carboxylic acid
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The invention discloses a method for preparing 2-methyl-4-(trifluoromethyl)thiazole-5-formyl acid. The method comprises the steps of synthesizing 2-bromo-trifluoro-ethyl acetoacetate and 2,2-dibromo-trifluoro-ethyl acetoacetate by reacting trifluoro ethyl acetoacetate with liquid bromine by using trifluoro ethyl acetoacetate as a raw material; then preparing ethyl acetoacetate of 2-methyl-4-(trifluoromethyl)thiazol-5-ethyl formate by reacting with an inert organic solvent solution of thioacetamide; and finally obtaining 2-methyl-4-(trifluoromethyl)thiazole-5-formyl acid by a hydrolysis reaction. The method has the advantages of novel raw materials and route, mild reaction conditions, simple operations, relatively high raw material conversion rate and product selectivity, convenient separation of target products, etc. The prepared 2-methyl-4-(trifluoromethyl)thiazole-5-formyl acid can be used for synthesizing a key intermediate of thiazole amide fungicides (thifluzamide).
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Paragraph 0033; 0034
(2016/11/21)
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- INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE
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The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below.
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Page/Page column 178
(2010/07/10)
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- Improved process for the preparation of thioacetamide
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An improved process for the reaction of acetonitrile and hydrogen sulfide to produce thioacetamide, wherein a polymer-supported amine catalyst is used. Examples of the polymer-supported amine catalyst are polymeric dimethylaminopyridine resins, poly(4-vinylpyridine) cross-linked with divinylbenzene, and cross-linked polymer-supported 4-(N-benzyl-N-methylamino)pyridine.
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- Process for the preparation of thioacetamide
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An improved process for the reaction of acetonitrile and hydrogen sulfide to produce thioacetamide, wherein a polymer-supported amine catalyst is used. Examples of the polymer-supported amine catalyst are polymeric dimethylaminopyridine resins, poly(4-vinylpyridine) cross-linked with divinylbenzene, and cross-linked polymer-supported 4-(N-benzyl-N-methylamino)pyridine.
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- Substituted thiazoles and their use as fungicides
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The present invention relates to certain substituted 5-carboxanilidothiazoles and their use as fungicides.
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- Thiazoles and pyrazoles as fungicides
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Heterocyclic derivatives represented by the following formula have excellent preventive, curative and systemic controlliing effects on various plant microbes. STR1 wherein R1 represents a hydrogen atom or a methyl group, A represents STR2 wherein R2 represents a methyl group, an ethyl group or a trifluoromethyl group, Y1 represents an amino group, a methyl group or a chlorine atom, R3 represents a methyl group or a trifluoromethyl group and Z represents a hydrogen atom, a halogen atom or a methyl group and when A represents the formula: STR3 X represents an oxygen atom or sulfur atom and when A represents the formula: STR4 X represents a sulfur atom.
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