- Method for preparing polysoproxil intermediate
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The method comprises the following steps: (1). A hydrogen chloride salt of 2 - chlorine -6 - methylaniline compound 1 is prepared by taking 2 - chlorine -6 - methylaniline compound 1 as a raw material in a suitable solvent, and then subjected to diazotization reaction with a nitration reagent aqueous solution to obtain the diazonium salt 2 - chloro -6 - methylaniline. The iodine-containing reagent is reacted with an iodo reagent to obtain 3 -chloro -2 -iodotoluene compound 2. (2), the compound 2 is reacted with the reactant cyanide to give 2 -chloro -6 -iodo-benzonitrile compound 3. (3), the compound 3 undergoes a hydrolysis reaction to obtain 2 - chloro -6 - methyl benzoic acid compound 4, and the reaction equation is as follows. The method has the advantages of cheap and easily available raw materials, high reaction conversion rate, simplicity and rapidness, mild and controllable reaction conditions, mild reaction conditions, high yield of the obtained product, easy separation and purification, high purity and easy industrial mass production.
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Paragraph 0034; 0082-0087
(2021/11/26)
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- Palladium-catalyzed highly selective ortho-halogenation (I, Br, Cl) of arylnitriles via sp2 C-H bond activation using cyano as directing group
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A palladium-catalyzed ortho-halogenation (I, Br, Cl) of arylnitrile is described. The optimal reaction conditions were identified after examining various factors such as catalyst, additive, solvent, and reaction temperature. Using cyano as the directing group, the halogenation reaction gave good to excellent yields. The method is compatible to the arylnitriles with either electron-withdrawing or electron-donating groups. The reaction is available to the substrate in at least gram scale. The present method was successfully applied to the synthesis of the precursors of paucifloral F and isopaucifloral F.
- Du, Bingnan,Jiang, Xiaoqing,Sun, Peipei
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p. 2786 - 2791
(2013/04/24)
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- 1,3-Dihydro-3-(2-hydroxy-, 2-bromo- or 2-chloroethyl)-2H-isoindol-1-one derivatives
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Derivatives of 1,3-dihydro-3-(2-hydroxyethyl) -2H-isoindol-1-one are disclosed. The derivatives are useful for treating ulcers in a mammal and for preventing or decreasing the secretion or availability of excessive amounts of gastric or hydrochloric acid in a mammal suffering from hyperchlorhydria and/or associated conditions.
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