- KAPPA OPIOID RECEPTOR ANTAGONISTS AND PRODUCTS AND METHODS RELATED THERETO
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Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: (I) wherein X, Y, R1, R2, R4, R5 R6, R7, R8 and R11 are as defined herein.
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Page/Page column 165; 166
(2018/10/19)
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- Method for the synthesis of many halo benzoic acid
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The invention provides a poly-halogenated benzoic acid synthesizing method. The method comprises the following steps: dissolving substituted benzoic acid, halogen and organic strong acid in a polar solvent for increasing temperature, after oxidation at a temperature of 50-70 DEG C, performing heat preservation at the temperature of 60-80 DEG C for 2-6 h, adding a right amount of water, and cooling to a room temperature, so as to obtain poly-halogenated benzoic acid. According to the invention, synthetic reaction is performed in an alcohols solvent, the halogen simple substance is used as a halogenating reagent, a small amount of organic strong acid is added, used as a catalyst, and used for catalyzing the electrophilic substitution reaction of the halogen to benzene rings, and hydrogen peroxide is dropwise added during the reaction to enable the halogen simple substance in the reaction system to be oxidized into halide ions so as to improve the utilization rate of the halogen and achieve the effect of atom economy.
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Paragraph 0041
(2017/04/03)
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