- A novel benzoyl pyrimidine urea compound and its preparation and use (by machine translation)
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The invention provides a benzoyl pyrimidine urea compound, of formula I or formula II structure shown. The present invention provides benzoyl pyrimidine urea compound has excellent armyworm killing, mosquito killing and broad-spectrum antifungal activity. The experimental result shows, the present invention provides benzoyl pyrimidine urea compound in 0.5 μg mL- 1 Sliding surface of larvae activity can be up to 100%, in the 0.25μg mL- 1 Sliding surface of larvae activity can be up to 100%. In the 50 μg mL- 1 When, demonstrated broad-spectrum antifungal activity, and to the cabbage in vitro blade has a certain protective effect. And low toxicity to fish, LC to the zebra fish50 Are respectively 378.387 mg L- 1 , 21.668 Mg L- 1 . Can be used to prepare insecticidal, anti-plant-pathogenic fungi pesticide application. (by machine translation)
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Paragraph 0058; 0059; 0060; 0062; 0065
(2019/01/06)
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- Investigation of novel pesticides with insecticidal and antifungal activities: Design, synthesis and SAR studies of benzoylpyrimidinylurea derivatives
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In order to find pesticides with insecticidal and antifungal activities, a series of novel benzoyl pyrimidinylurea derivatives were designed and synthesized. All target compounds were identified by 1H-NMR spectroscopy and HRMS. Insecticidal and antifungal activity of these compounds were evaluated and the structure-activity relationships (SAR) were clearly and comprehensively illustrated. Compound 7, with low toxicity to zebrafish (LC50 = 378.387 μg mL?1) showed 100% inhibition against mosquito (Culex pipiens pallens) at 0.25 μg mL?1. Both compounds 19 and 25 exhibited broad-spectrum fungicidal activity (>50% inhibitory activities against 13 phytopathogenic fungi), which were better than those of the commercial pesticide pyrimethanil (>50% inhibitory activities against eight phytopathogenic fungi). Furthermore, compounds 19 and 25 exhibited protective activity against Sclerotinia sclerotiorum on leaves of Brassica oleracea L. during in vivo experiments.
- Chen, Peiqi,Song, Xiangmin,Fan, Yongmei,Kong, Weihao,Zhang, Hao,Sun, Ranfeng
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- 2-amino-6-methoxypyrimidine-4-ol preparation process
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The invention discloses a 2-amino-6-methoxypyrimidine-4-ol synthesis process. 4,6-dichloropyrimidine-2-amine is used as a starting material to obtain 2-amino-6-methoxypyrimidine-4-ol through a three-step reaction which includes nucleophilic substitution, electrophilic substitution and catalytic hydrogenation. The synthesis method has advantages of cheapness and easiness in acquisition of raw materials, mild operation conditions, simplicity, convenience and feasibility in aftertreatment and suitableness for industrial application.
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Paragraph 0005; 0027; 0028
(2017/08/29)
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- POLYMER FILM, RETARDATION FILM, POLARIZING PLATE, LIQUID CRYSTAL DISPLAY, AND COMPOUND
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Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Qa, Qb, and Qc are a single bond or a divalent linking group. Ra, Rb, and Rc, are hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, cyano group, halogen group, or heterocyclic group. X2 is a single bond or a divalent linking group. X1 is a single bond or a predetermined divalent linking group. R1 and R2 are a hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, or heterocyclic group Formula (1)
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Paragraph 0400
(2016/06/28)
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- DI(HETERO)ARYLAMIDES AND SULFONAMIDES, METHODS FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF
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The present invention refers to compounds of formula (I): as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of conditions associated with the alteration of the activity of β-galactosidase, specially galactosidase beta-1 or GLB1, including GM1 gangliosidoses and Morquio syndrome, type B.
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Page/Page column 64
(2015/02/25)
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- Identification of NVP-BKM120 as a potent, selective, orally bioavailable class i PI3 kinase inhibitor for treating cancer
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Phosphoinositide-3-kinases (PI3Ks) are important oncology targets due to the deregulation of this signaling pathway in a wide variety of human cancers. Herein we describe the structure guided optimization of a series of 2-morpholino, 4-substituted, 6-heterocyclic pyrimidines where the pharmacokinetic properties were improved by modulating the electronics of the 6-position heterocycle, and the overall druglike properties were fine-tuned further by modification of the 4-position substituent. The resulting 2,4-bismorpholino 6-heterocyclic pyrimidines are potent class I PI3K inhibitors showing mechanism modulation in PI3K dependent cell lines and in vivo efficacy in tumor xenograft models with PI3K pathway deregulation (A2780 ovarian and U87MG glioma). These efforts culminated in the discovery of 15 (NVP-BKM120), currently in Phase II clinical trials for the treatment of cancer.
- Burger, Matthew T.,Pecchi, Sabina,Wagman, Allan,Ni, Zhi-Jie,Knapp, Mark,Hendrickson, Thomas,Atallah, Gordana,Pfister, Keith,Zhang, Yanchen,Bartulis, Sarah,Frazier, Kelly,Ng, Simon,Smith, Aaron,Verhagen, Joelle,Haznedar, Joshua,Huh, Kay,Iwanowicz, Ed,Xin, Xiaohua,Menezes, Daniel,Merritt, Hanne,Lee, Isabelle,Wiesmann, Marion,Kaufman, Susan,Crawford, Kenneth,Chin, Michael,Bussiere, Dirksen,Shoemaker, Kevin,Zaror, Isabel,Maira, Sauveur-Michel,Voliva, Charles F.
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supporting information; experimental part
p. 774 - 779
(2011/12/03)
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- PI 3-KINASE INHIBITORS AND METHODS OF THEIR USE
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Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, auutoimmune and cardiovascular diseases.
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Page/Page column 65
(2008/12/08)
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- PYRIMIDINE DERIVATIVES USED AS PI-3 KINASE INHIBITORS
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Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof ; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.
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Page/Page column 98-99
(2010/11/28)
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- METHOD FOR THE PRODUCTION OF 2-AMINO-4-CHLORO-6-ALKOXYPYRIMIDINES
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The invention relates to a method for producing 2-amino-4-chloro-6-alkoxypyrimidines by reacting 2-amino-4,6-dichloropyrimidine with an alkali alcoholate or a mixture of alkali hydroxides and an alcohol in a polar aprotic solvent (mixture), whereupon the solvent is distilled off to > 30 percent and the product is precipitated by adding water during or following the distillation process. The inventive method, in which especially acetone is used as a polar aprotic solvent and which can be carried out at temperatures between 5 and 60 °C, allows 2-amino-4-chloro-6-alkoxypyrimidines and above all 2-amino-4-chloro-6-methoxypyrimidine to be produced in a particularly economical and environmentally friendly manner while obtaining high yields and a very distinctive purity.
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Page/Page column 6-7
(2008/06/13)
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- Phototransformation of Chlorimuron-ethyl in Aqueous Solution
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Chlorimuron-ethyl is relatively stable in water buffered to pH 7.0 and 9.0, but hydrolyzes readily (half-life, 14 d) in water buffered to pH 4.0. In addition, chlorimuron-ethyl photodegrades rapidly and extensively in aqueous solution. The predominant photoproducts are 4-methoxy-6-chloro-2-aminopyrimidine, ethyl 2-aminosulfonylbenzoate, N-(4-methoxy-6-chloropyrimidin-2-yl)methyl urea, and o-benzoic sulfimide (saccharin). A minor deesterified product (chlorimuron) was evident. The decrease in chlorimuron-ethyl concentration in aqueous solutions followed first-order kinetics. The rate of degradation in different types of water followed the order irrigation water > tap water > distilled water. Chlorimuron-ethyl photodegraded in pH 4, 7, and 9 buffer solutions under both UV and sunlight. A faster degradation rate in pH 4.0 buffer solution was observed.
- Choudhury, Partha P.,Dureja, Prem
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p. 3379 - 3382
(2007/10/03)
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- Dimethoxypyrimidines as Novel Herbicides. Part 1. Synthesis and Herbicidal Activity of Dimethoxyphenoxypyrimidines and Analogues
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A number of 6-(4-phenoxyphenoxy)pyrimidines and triazines were synthesized and their herbicidal activity was measured. Compounds with the methoxy groups at the 2- and 4-positions on the pyrimidine and triazine rings exhibited high herbicidal activity. Introduction of a substituent into the 5-position of the pyrimidine ring diminished the activity. In the phenoxyphenoxy substructure at the 6-position, the central ether bond can be replaced by a methylene group without loss of activity. The optimum substituent on the terminal phenyl ring was 3-trifluoromethyl. The compounds showed a strong Hill reaction inhibition, but unfortunately showed poor selectivity between weeds and crops. - Keywords: phenoxyphenoxypyrimidines; phenoxyphenoxy-s-triazines; Hill reaction inhibitors; 2,6-dimethoxy-4-pyrimidine; 2,6-dimethoxy-4--s-triazine; herbicides
- Nezu, Yukio,Miyazaki, Masahiro,Sugiyama, Kazuhiko,Kajiwara, Ikuo
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p. 103 - 114
(2007/10/03)
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- Process for producing sulfonylureas
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There is described a novel process for producing sulfonylureas of formula I STR1 wherein R1 is hydrogen or alkyl, R2 is STR2 E is =N-- or =CH--, R3 is alkyl, alkoxy or halogen, R4 is alkyl, cycloalkyl, alkoxy, halogen, alkoxy-alkyl, halo-alkyl or halo-alkoxy, R5 is hydrogen or alkyl, T is a substituted phenyl group STR3 Y is hydrogen or halogen, X is hydrogen, halogen, alkyl, halo-alkyl, alkenyl, halo-alkenyl, alkynyl, alkoxy, halo-alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halo-alkylthio, alkylsulfonyloxy, phenylsulfonyloxy, phenylsulfonyloxy mono- or polysubstituted by alkyl, or is di-alkylsulfamoyl, and A is a bridge member which has 3 or 4 atoms and which contains 1 or 2 hetero atoms, selected from the group consisting of oxygen, sulfur and nitrogen, the said process comprising reacting a silfonamide of the formula II in the presence of a base, with diphenyl carbonate to form a salt of a phenyl carbamate converting this salt into the free phenyl carbamate and reacting this further with an amine. Sulfonylureas are herbicidally effective compounds.
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- Herbicidal sulfonamides
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This invention relates to novel sulfonamides, agriculturally suitable compositions containing them and their method-of-use as selective pre-emergent or post-emergent herbicides.
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- Herbicidal sulfonamides
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This invention relates to novel sulfonamides, agriculturally suitable compositions containing them and their method-of-use as selective pre-emergent or post-emergent herbicides.
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