- FUROINDAZOLE DERIVATIVES
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The present invention covers furoindazole compounds of general formula (I): in which (I) are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of autoimmune diseases such as multiple sclerosis, psoriasis, psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis, systemic lupus erythematosus, primary and secondary autoimmune uveitis, inflammatory disorders like endometriosis, inflammatory eye diseases, inflammatory kidney diseases, inflammatory liver diseases like non-alcoholic, alcoholic- and toxic fatty liver diseases, lung diseases like asthma, idiopathic pulmonary fibrosis, chronic obstructive pulmonary disease and metabolic and metabolic-endocrine disorders like metabolic syndrome, insulin resistance, diabetes mellitus type I and type II, and polycystic ovary syndrome (PCOS) disorders, neuropathic and inflammatory pain disorders in humans and animals.
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Page/Page column 116; 117
(2021/06/26)
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- Chalcone compound and applications thereof
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The present invention relates to a chalcone-containing compound represented by a general formula (I), and a pharmaceutically acceptable salt, a solvate and a prodrug thereof, wherein the substituentsR1, R2, R3, R4, R5, R6, Q and n have the meanings given in the specification. The invention further relates to applications of the compound represented by the general formula (I) in preparation of anti-tumor drugs, and applications of the compound and the pharmaceutically acceptable salt, solvate and prodrug thereof in preparation of drugs for preventing and/or relieving cancers caused by tumor cells of human tissues or organs, wherein the cancers are preferably colon cancer, liver cancer, lymphoma, lung cancer, esophageal cancer, breast cancer, central nervous system tumor, melanoma, skin cancer, ovarian cancer, cervical cancer, kidney cancer, leukemia, prostate cancer, pancreatic cancer, bladder cancer, rectal cancer, osteosarcoma, nasopharyngeal cancer, gastric cancer and the like.
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Paragraph 0115; 0116; 0117
(2020/06/17)
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- Iodine-containing pyrazinamide compound, preparation method and applications thereof, and bactericide
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The present invention relates to the field of pesticide bactericides, and discloses an iodine-containing pyrazinamide compound, a preparation method and applications thereof, and a bactericide, wherein the compound has a structure represented by a formula (I). According to the present invention, the iodine-containing pyrazinamide compound with the completely-new structure is designed by introducing the pyrazine ring of NNF-0721 and the diphenyl ether fragment having broad biological activity, and can be used as the completely-new succinate dehydrogenase inhibitor or bactericide. The formula (I) is defined in the specification.
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Paragraph 0044; 0057-0058
(2019/05/02)
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- Pyrazinamide compound, preparation method and applications thereof, and bactericide
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The present invention relates to the field of pesticide bactericides, and discloses a pyrazinamide compound, a preparation method and applications thereof, and a bactericide, wherein the compound hasa structure represented by a formula (I). The preparatio
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Paragraph 0115-0116
(2019/11/04)
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- Preparation method of ethyl 2-chloro-4,4,4-trifluoroacetoacetate
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The invention belongs to the technical field of pesticide chemistry and particularly relates to a preparation method of ethyl 2-chloro-4,4,4-trifluoroacetoacetate. Ethyl trifluoroacetoacetate is usedas a raw material subjected to substitution reaction with sulfonyl chloride before distilling under maintained temperature and reduced pressure is performed to obtain ethyl 2-chloro-4,4,4-trifluoroacetoacetate. A sulfur-bearing lubricant additive is used as a catalyst; reaction temperature is lowered; reaction time is shortened; the quantity of polychlorinated products is reduced; the conversion rate of ethyl trifluoroacetoacetate is >/=99%, product yield is above 93%, and the purity is above 98%.
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Paragraph 0024-0053
(2019/04/17)
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- Trifluoromethyl-containing pyrazinamide compound, preparation method and applications thereof, and bactericide
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The present invention relates to the field of pesticide bactericides, and discloses a trifluoromethyl-containing pyrazinamide compound, a preparation method and applications thereof, and a bactericide, wherein the compound has a structure represented by a
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Paragraph 0058-0059
(2019/05/02)
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- Design, synthesis, insecticidal, and acaricidal activities of novel pyrimidinamine derivatives containing a biphenyl ether
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A series of original pyrimidinamine derivatives containing a biphenyl ether moiety were designed and synthesized. Their structures were confirmed by 1H NMR, MS, and elemental analyses. Their insecticidal activities against lepidopteran and hemiptera insects and acaricidal activities were tested. The results of bioassay demonstrated that 9k showed the best activity (LC50 = 2.08 mg/L) against Tetranychus urticae, which is comparable with the positive control, spirotetramat (LC50 = 2.27 mg/L), and 9g showed better activity (LC50 = 0.52 mg/L) against Aphis fabae than the positive control, imidacloprid (LC50 = 1.02 mg/L), and relatively good activity (LC50 = 2.49 mg/L) against T urticae. Their structure-activity relationships indicated that both an ethyl group on the 4-position of the pyrimidine ring and alkyl chain as a para-substituent group of the benzene ring showed good biological activity.
- Li, Lizhong,Zhou, Chunge,Liu, Minhua,Zhang, Ping,Zhang, Ning,Li, Jianming,Li, Tao,Liu, Xingping,Cheng, Shufen,Li, Qianhe,Liu, Aiping
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p. 3206 - 3214
(2019/11/13)
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- Pyrazinamide compounds, preparation method and application thereof as well as bactericide
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The invention relates to the field of pesticide bactericides and discloses pyrazinamide compounds, a preparation method and an application thereof as well as a bactericide. The compounds have the structure shown in formula (I). The pyrazinamide compounds with the novel structure are designed by introducing pyrazine ring fragments in Pyradiflumid and diphenyl ether fragments with wide bioactivity,and the pyrazinamide compounds can be used as novel SDHIs (succinate dehydrogenase inhibitors) or bactericides.
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Paragraph 0133; 0134
(2018/06/04)
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- Pyrazinamide compounds and preparing method and application thereof and bactericide
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The invention relates to the field of pesticide bactericides, and discloses a pyrazinamide compound and a preparing method and application thereof and a bactericide. The pyrazinamide compound has thestructure shown in the formula (I) or the formula (II) or the formula (III). According to the pyrazinamide compound and the preparing method and application thereof and the bactericide, by introducingpyrazine ring fragments and and diphenyl ether fragments with the wide biological activity in NNF-0721, and the pyrazinamide compound with the brand-new structure is designed; the pyrazinamide compound can serve as a brand-new succinodehydrogenase inhibitor or a bactericide. The formula is defined in the description.
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Paragraph 0120; 0135; 0136
(2019/01/14)
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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 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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- Design, synthesis and antifungal activity of new substituted difluoromethylpyrimidinamine derivatives
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Rusts are one of the most important fungal diseases, the known target sites have already developed serious resistance to the main existing classifications of fungicides. In order to discover novel fungicides with a promising activity on rusts, twenty new substituted difluoromethylpyrimidinamine derivatives were designed and synthesized with the aid of the intermediate derivatization methods starting from ethyl 4,4-difluoro-3-oxobutanoate that is the common raw material in some newly launched important succinate dehydrogenase inhibitor (SDHI) fungicides. Their structures were identified by 1H NMR, 13C NMR, 19F NMR, IR, elemental analyses and HRMS. All the compounds were screened for in vivo fungicidal activity against southern corn rust (SCR). The preliminary bioassay results indicated that 5-chloro-6-(difluoromethyl)-N-(2-(6-(3-(trifluoromethyl)phenoxy)pyridin-3-yl)ethyl)pyrimidin-4-amine (compound J, R1 = CHF2, Alk = CH2CH2, Rn = 3-CF3) is the optimal structure with desired fungicidal activity against SCR (EC50 = 2.16 mg/L), significantly higher than commercial fungicides diflumetorim (EC50 = 53.26 mg/L) and propiconazole (EC50 = 3.92 mg/L). The structure–activity relationship of the synthesized compounds was discussed as well. This study also demonstrated that difluoromethylpyrimidinamine derivatives can be further utilized as a promising antifungal agent to control rust. Further synthesis and structure optimization studies are currently in progress.
- Guan, Aiying,Wang, Mingan,Chen, Wei,Yang, Fan,Yang, Jinlong,Zhao, Yu,Li, Zhinian,Liu, Changling
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- A kind of 3,4-dichloro-thiazole derivatives and process for their preparation and use
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The invention provides 3,4-dichloro isothiazole derivatives, their preparation method and application. The invention relates to a heterocyclic compound containing 3,4-dichloro isothiazol, and the compound is represented by the following chemical structural general formula. The invention discloses the structural general formula of the compound, a synthetic method of the compound and applications of the compound as pesticide, bactericide, anti-plant virus agent, and plant activator, and a technology of mixing the compound with agriculturally acceptable auxiliary agents or synergists for preparing pesticide, bactericide, anti-plant virus agent, and plant activator. The invention further discloses the combined application of the compound and the commercial pesticide, bactericide, anti-plant virus agent, and plant activator in controlling diseases, insect pests, and virus diseases in agriculture, forestry and gardening, and a preparation method of the compound and the commercial pesticide, bactericide, anti-plant virus agent, and plant activator.
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Paragraph 0050-0051; 0097-0098
(2016/10/08)
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- Synthesis and Biological Activity of Ethyl 4-Alkyl-2-(2-(substituted phenoxy)acetamido)thiazole-5-carboxylate
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(Chemical Equation Presented) A series of novel ethyl 4-(methyl or trifluoromethyl)-2-(2-(substituted phenoxy)acetamido)thiazole-5-carboxylates 7a, 7b, 7c, 7d, 7e and 8f, 8g, 8h, 8i, 8j, 8k, 8l, 8m, 8n, 8o, 8p, 8q, 8r were synthesized, and their structures were confirmed by IR, 1H-NMR, MS spectra and elemental analysis. The results of preliminary bioassays show that some of the title compounds exhibit moderate to good herbicidal activities. Compared with the fluorine free compounds 7a, 7b, and 7e, the compounds bearing fluorine 8g, 8j, and 8q showed higher herbicidal activities with 70-100% inhibition against Capsella bursa-pastoris, Amaranthus restroflexus, and Eclipta prostrata at the dosage of 150 g/ha, which indicated that the trifluoromethyl on the thiazole ring was beneficial for the herbicidal activity. Furthermore, compounds 8f, 8g, 8h, 8i, 8j, 8k, 8l, 8m, 8n, 8o, 8p, 8q, 8r were tested for fungicidal activity against Pseudoperonospora cubensis at 500 μg/mL. Compounds 8f and 8q showed the best fungicidal activity with more than 80% inhibition.
- Mo, Wenyan,Shi, Yanxia,He, Junbo,Li, Baoju,Peng, Hao,He, Hongwu
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p. 183 - 187
(2016/02/10)
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- A containing [...] the carboxamide derivative and its preparation and application (by machine translation)
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This invention relates to a kind of the carboxamide derivatives containing [...] and its preparation method and application. The oxalyl chloride, benzoic acid and ammonia-water reaction to make compound VI-1; compound VI-1 and olausson reagent reaction synthesis of compound VI-2; ethyl acetate to trifluoroacetoacetic reaction of the sulfonyl chloride compound VI-3; compound VI-2 and VI-3 VI-4 reaction to obtain compound, compound VI-4 with methanol, sodium hydroxide reaction to make compound VI-5; compound VI-5 with anthranilic acid amide, acid the system results in the type pyridine (I); the simple and easily-obtained raw materials, the preparation method is simple, convenient post-treatment, the product yield is high, and the compound is having a bactericidal activity, against cucumber gray mold, cucumber most bacterial corner sclerostachya sickness and so on and has good effect for of, but also has anti-cancer activity, the research and development of new drug is providing the foundation. (by machine translation)
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Paragraph 0007; 0016
(2016/10/31)
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- Halogenation of fluorinated cyclic 1,3-dicarbonyl compounds: new aspects of synthetic application
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In order to elaborate on an approach towards 2-(fluoroacyl)phenols being the superior alternative to the conventional Fries-rearrangement based methodology, the behaviour of cyclic fluorinated 1,3-dicarbonyls in reactions with halogenating agents was examined. The synthetic relevance of the polyhalogenated compounds obtained was demonstrated by the synthesis of several new heterocycles. An aromatization via a halogenation-dehydrohalogenation sequence proved to be a rewarding synthetic route to 2-(fluoroacyl)phenols and previously unknown 3-(fluoroacyl)thiochromones. The structure of one of the synthesized compounds was confirmed by X-ray diffraction analysis.
- Sevenard, Dmitri V.,Vorobyev, Mikhail,Sosnovskikh, Vyacheslav Ya.,Wessel, Helma,Kazakova, Olesya,Vogel, Vera,Shevchenko, Nikolay E.,Nenajdenko, Valentine G.,Lork, Enno,R?schenthaler, Gerd-Volker
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experimental part
p. 7538 - 7552
(2009/12/06)
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- 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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p. 1287 - 1290
(2007/10/03)
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- 5-carboxanilido-2,4-bis-trifluoromethylthiazoles and their use to control rice blast
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The present invention provides 5-carboxanilido-2,4-bis-trifluoromethylthiazoles and their compositions. The compounds and compositions are effective for controlling fungal diseases on plants. They are particularly effective for controlling rice blast.
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Page column 4
(2008/06/13)
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- 5-Carboxanilido-haloalkylthiazoles as antimicrobial and marine antifouling agents
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The present invention relates to a method for inhibiting the growth of microorganisms and marine organisms at a locus. In particular, the present invention relates to the use of certain 5-carboxanilido-haloalkylthiazoles as antimicrobial and marine antifouling agents.
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- Microbicidal salts of 5-carboxanilido-haloalkylthiazoles
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Compounds of the formula:whereinA is a strong base cation;R1and R2are independently (C1-C5)alkyl or (C1-C2)haloalkyl, provided that at least one of R1and R2is (C1-C2)haloalkyl;each R is independently halo, halo(C1-C5)alkyl, halo(C1-C5)alkoxy, nitro, cyano, pentahalosulfur, halomethylthio, haloethylthio, (C1-C2)alkylsulfinyl, halo(C1-C2)alkylsulfinyl, (C1-C2)alkylsulfonyl, or halo(C1-C2)alkylsulfonyl; andn is from one to five,are useful as fungicides, microbicides, marine antifoulants, and termiticides, compositions containing those compounds, and methods for their use.
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- Synthesis of trifluoromethylated dihydro-1,4-oxathhn-3-carboxanilides through polymer-bound activated ester
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A synthesis of new trifluoromethylated dihydro-1,4-oxathiin-3-carboxanilids (2) through polymer-bound activated ester is described. Chlorination of ethyl γ,γ,γ-trifluoroacetoacetate (3) followed by treatment of 2-mercaptoethanol gave hydroxyoxathianes isomers (cis-10 and trans-11). Replacement of hydroxy to chlorine and then dehydrochlorination afforded trifluoromethyl dihydro-1,4-oxathiin ester (7). The polymer-bound trifluoromethylated dihydro-1,4-oxathiin-3-carboxylic acid, 4-hydroxy-3-nitrobenzophenone ester (16) was prepared through the reaction of polystyrene-bound 4-hydroxy-3-nitrobenzophenone (14) with the trifluoromethylated dihydro-1,4-oxathiin-3-carbonyl chloride (15). Refluxing of 16 with anilines in acetonitrile gave the corresponding carboxanilide (2). The reaction rate depended on the nucelophilicity of nitrogen in aniline.
- Hahn, Hoh-Gyu,Chang, Kee Hyuk,Nam, Kee Dal,Bae, Su Yeoul,Mah, Heduck
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p. 2253 - 2261
(2007/10/03)
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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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