- Synthesis and Fungicidal Activity of Novel 2-Heteroatomthiazole-based Carboxanilides
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A new series of 2-heteroatomthiazole-based carboxanilides (8) are prepared by reacting 2-heteroatomthiazole-based carboxylic acid chlorides with 2,6-dibromo-4-(trifluoromethoxy)aniline. The structures of all the newly synthesized compounds were supported by spectroscopic data NMR, MS, and elemental analysis, etc. Bioassay showed that the compounds exhibited potent fungicidal activities against Rhizoctonia solani, etc. Particularly, N-(2,6-dibromo-4-(trifluoromethoxy)phenyl)-2-methoxy-4-(trifluoromethyl)thiazole-5-carboxamide (8a-2) showed fungicidal potency which was comparable to that of Thifluzamide, the only commercialized thiazole carboxanilide fungicides of succinate dehydrogenase inhibitor (SDHI).
- Liu, Aiping,Wang, Xiaoguang,Liu, Xingping,Li, Jianming,Chen, Haobin,Hu, Li,Yu, Wanqi,He, Lian,Liu, Weidong,Huang, Mingzhi
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p. 1625 - 1629
(2017/03/27)
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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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- Synthesis of 2-(Benzylthio)-4-(trifluoromethyl)thiazole-5-carboxylates Using S -Benzylisothiouronium Halides as Thiol Equivalents
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S-Benzylisothiouronium halides are used as shelf-stable, odorless thiol equivalents. The method developed is used to access 2-(benzylthio)-4-(trifluoromethyl)thiazole carboxyl building blocks. Using the latent trifluoromethyl substituent the reactions could be monitored using 19F NMR spectroscopy.
- Hickey, Shane M.,White, Jonathan M.,Pfeffer, Frederick M.,Ashton, Trent D.
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supporting information
p. 1759 - 1763
(2015/07/20)
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- SUBSTITUTED BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
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- AMIDE COMPOUND
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A compound represented by the formula (I) wherein ring Cy1 is a 5-membered aromatic heterocycle optionally further substituted besides a group represented by -A-B, ring Cy2 is an optionally substituted benzene ring, ring Cy3 is an optionally substituted 5-membered aromatic heterocycle, ring Cy4 is an optionally substituted 6-membered aromatic ring, A is -CONRa- or -NRaCO-, Ra is a hydrogen atom or a substituent, B is a hydrogen atom or an optionally substituted C1-6 alkyl-group, X is an optionally substituted C1-2 alkylene, -Y-, -Y-CH2- or - CH2-Y-, Y is an oxygen atom, -NRb- or -S(O)m-, Rb is a hydrogen atom or a substituent, and m is 0, 1 or 2, provided that N-methyl-4-[2-[3,4,5-trimethoxyphenyl)amino]-1,3-benzoxazol-7-yl]thiophene-2-carboxamide is excluded, or a salt thereof, has an agonistic action on GPR52, and is useful as an agent for the prophylaxis or treatment of schizophrenia and the like.
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Page/Page column 54
(2012/11/13)
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- 5-MEMBERED HETEROCYCLIC AMIDES AND RELATED COMPOUNDS
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5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly usef
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Page/Page column 97
(2009/03/07)
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- Synthesis of 2-aminoethyl-5-carbethoxythiazoles utilizing a Michael-like addition strategy
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Ethyl 4-(trifluoromethyl)-2-vinylthiazole-5-carboxylate was utilized as a precursor to ethyl 4-(trifluoromethyl)-2-(aminoethyl)thiazole-5-carboxylate analogs via Michael-like addition of various secondary amines. Reactions employed 1.2 equiv of amine, and the products were isolated by solvent removal and acid/base extraction. Use of primary amines was also investigated.
- Boy, Kenneth M.,Guernon, Jason M.
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p. 2251 - 2252
(2007/10/03)
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- Aminoalkyl thiazole derivatives as KCNQ modulators
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Novel aminoalkylthiazole derivatives of Formula I are described which are openers of KCNQ potassium channels and are useful in the treatment of disorders responsive to the opening of the KCNQ potassium channels, including pain and migraine.
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- 2-aryl thiazole derivatives as KCNQ modulators
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Novel 2-arylthiazole derivatives of Formula I are described which are openers of KCNQ potassium channels and are useful in the treatment of disorders that are responsive to the opening of the KCNQ potassium channels, including pain and migraine.
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- Syntheses and Reactions of 2-Halo-5-thiazolecarboxylates
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A variety of 2-halo-5-thiazolecarboxylates was prepared from substituted-3-aminoacrylates and 3-ketoesters.Selective reduction of 2-chloro-5-thiazolecarboxylates 4a, 4i and 4j with sodium borohydride in ethanol provided the corresponding 2-halo-5-thiazolemethanols 27 - 29.Nucleophilic displacement on methyl methanesulfonate (32c) occured selectivity at the 5-substituent to provide 2-chloro-4-(trifluoromethyl)-5-(heteroatom-substituted methyl)thiazoles 32d-f.
- Lee, Len F.,Schleppnik, Francis M.,Howe, Robert K.
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p. 1621 - 1630
(2007/10/02)
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- 2,4-Disubstituted-5-thiazole-carboxylic acids and derivatives
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2,4-Disubstituted-5-thiazolecarboxylic acids and derivatives thereof have been found to reduce herbicidal injury of corn, rice and sorghum plants due to the application thereto of acetamide herbicides.
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- 2,4-Disubstituted-5-thiazole-carboxylic acids and derivatives
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2,4-Disubstituted-5-thiazolecarboxylic acids and derivatives thereof have been found to reduce herbicidal injury of corn, rice and sorghum plants due to the application thereto of acetamide herbicides.
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- 2,4-Disubstituted-5-thiazolecarboxylic acids and derivatives
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2,4-Disubstituted-5-thiazolecarboxylic acids and derivatives thereof have been found to reduce herbicidal injury of corn, rice and sorghum plants due to the application thereto of acetamide herbicides.
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