- PROCESS FOR THE PREPARATION OF CHLORANTRANILIPROLE
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The present invention relates to two novel, efficient and one-pot methods for synthesizing chlorantraniliprole. In the first scheme, Chlorantraniliprole is prepared by a novel telescopic process starting from 3-Bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxylic acid a key raw material-A (Key RM-A). In the second scheme, starting from Key RM-A, the process steps use of a novel variant of anthranilic acid (Methyl 2-amino-5-chloro-3-methylbenzoate), to get Chlorantraniliprole. Furthermore, the present invention also relates to the synthesis of key starting material for the synthesizing chlorantraniliprole in-situ. All the in-situ steps of the disclosed synthesis methods obtain good yield, without using any expensive reagent or base or harsh reaction conditions, which makes the process simple, environment friendly and more cost effective. With this process the production cost of chlorantraniliprole and its intermediates is substantially reduced; fewer by-products are formed during its synthesis and since it's a one-pot reaction, isolation and purification are easy to achieve.
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Page/Page column 9; 17-18
(2021/02/26)
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- PROCESS FOR PREPARATION OF ARTHROPODICIDAL ANTHRANILAMIDE COMPOUNDS
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The present invention provides a process for preparation of arthropodicidal anthranilamide compounds. The present invention further relates to one pot process for preparation of anthranilamide compounds.
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Page/Page column 21-22
(2021/08/20)
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- Preparation method of 2-amino-5-chloro-N, 3-dimethylbenzamide
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The invention relates to a preparation method of 2-amino-5-chloro-N, 3-dimethylbenzamide. The preparation method comprises the following steps: taking 2-nitro-3-methylbenzoic acid as an initial raw material, and sequentially carrying out a reduction reaction, a chlorination reaction, an esterification reaction and an ammonolysis reaction, so as to obtain 2-amino-5-chloro-N, 3-dimethylbenzamide. The preparation method provided by the invention provides a new path for synthesis of 2-amino-5-chloro-N, 3-dimethylbenzamide, the yield of the whole path can reach 80% or above, the cost is significantly reduced, the reaction conditions of each step are mild, the number of three wastes is small, and the method is suitable for industrial production.
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- 2-amino-5-chloro-N,3-dimethylbenzamide preparation method
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The invention discloses a 2-amino-5-chloro-N,3-dimethylbenzamide preparation method, which comprises: carrying out a chlorination reaction a raw material represented by a formula I and a chlorinationreagent at the ortho-position and the para-position of amino to generate a compound represented by a formula II, carrying out a selective substitution reaction on the compound represented by the formula II and a cyano group mainly based on amino o-chlorine substitution under an alkaline catalysis condition by utilizing the thermodynamic stability difference between the o-chlorine and the p-chlorine of amino to generate a compound represented by a formula III, hydrolyzing the compound represented by the formula III into a compound represented by a formula IV, esterifying the compound represented by the formula IV to generate a compound represented by a formula V, and carrying out a reaction on the compound represented by the formula V and a monomethylamine methanol solution to generate 2-amino-5-chloro-N,3-dimethylbenzamide. According to the invention, the preparation method is high in yield, simple in reaction and small in toxic and side effects.
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- Asymmetric Synthesis of Fused Polycyclic Indazoles through Aminocatalyzed Aza-Michael Addition/Intramolecular Cyclization
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The first example of an asymmetric aminocatalyzed aza-Michael addition of 1H-indazole derivatives to α,β-unsaturated aldehydes is described. The iminium/enamine cascade process lies at the heart of our strategy, leading to enantioenriched fused polycyclic indazole architectures. Variations on both the α,β-unsaturated aldehydes and the indazole-7-carbaldehyde heterocycles were studied in order to broaden the scope of the transformation in synthetically interesting directions. The fused polycyclic indazoles exhibit fluorescence properties and can undergo synthetic transformations.
- Giardinetti, Maxime,Marrot, Jér?me,Moreau, Xavier,Coeffard, Vincent,Greck, Christine
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p. 6855 - 6861
(2016/08/16)
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- POLYSUBSTITUTED PYRIDYL PYRAZOLECARBOXAMIDE AND PREPARATION METHOD AND USE THEREOF
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The present invention discloses a polysubstituted pyridyl pyrazolecarboxamide and its preparation method and use. The structure of the polysubstituted pyridyl pyrazolecarboxamide of the present invention is shown in the following General Formula I. The po
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Paragraph 0057; 0058; 0059
(2015/11/28)
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- COMPOUNDS AND METHODS FOR ANTIVIRAL TREATMENT
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Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections
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Paragraph 0796-0799
(2013/10/22)
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- Design, synthesis and biological activities of novel anthranilic diamide insecticide containing trifluoroethyl ether
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Two series of novel anthranilic diamide insecticide containing trifluoroethyl ether were designed and synthesized, and their structures were characterized by 1H NMR spectroscopy, elemental analysis and single crystal X-ray diffraction analysis. The insecticidal activities of the new compounds were evaluated. The results of bioassays indicated that some of these title compounds exhibited excellent insecticidal activities. The insecticidal activities of compounds 19a, 19b, 19d, 19g, 19k and 19m against oriental armyworm at 2.5 mg·kg-1 were 100%. The larvicidal activities of 19a, 19b, 19c, 19d, 19e, 19g and 19n against diamond-back moth were 100% at 0.1 mg·kg-1. Surprisingly, most of them still exhibited perfect insecticidal activity against diamond-back moth when the concentration was reduced to 0.05 mg·kg-1, which was higher than the commercialized Chlorantraniliprole.
- Zhao, Yu,Li, Yongqiang,Xiong, Lixia,Wang, Hongxue,Li, Zhengming
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p. 1748 - 1758
(2012/11/13)
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- PYRAZOLO [1, 5 -A] PYRIMIDINES AS ANTIVIRAL AGENTS
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The invention provides compounds of Formula I or Formula II: (I), (II) or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
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Page/Page column 296
(2012/01/14)
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- METHOD FOR PREPARING N-PHENYLPYRAZOLE-1-CARBOXAMIDES
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A method is disclosed for preparing compounds of Formula (I) by combining compounds of Formulae (II and III) and a sulfonyl chloride. Also disclosed are compounds of Formula (III), which are useful as starting materials for this method.
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Page/Page column 23
(2008/06/13)
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