- Synthesis method of 2,3,4-trihydroxybenzophenone
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The invention relates to a preparation method of polyhydroxy benzophenone, and concretely relates to a synthesis method of 2,3,4-trihydroxybenzophenone. The invention aims to solve the technical problems of complex operation, long reaction time and certain difficulty in an industrialization process when 2,3,4-trihydroxybenzophenone is prepared in the prior art. The synthesis method of 2,3,4-trihydroxybenzophenone comprises the following steps: adding pyrogallol and benzoic acid as raw materials into a solvent, heating to 80-140 DEG C under the action of a catalyst, separating water until no water is separated out, carrying out a heat preservation reaction, cooling to 60-100 DEG C after the reaction is finished, filtering out the catalyst, cooling to 0-60 DEG C, and filtering out the product; and continuously adding the solvent, phloroglucinol and benzoic acid into the filtered catalyst and mother liquor of the product, and repeating the reaction. The method has the following characteristics: the operation is simple, the environmental pollution is small, the requirement on equipment is low, no metal ions are introduced or used in the whole process, and the synthesized 2,3,4-trihydroxybenzophenone meets the manufacturing requirement of microelectronic circuit products.
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Paragraph 0031-
(2020/06/17)
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- Evaluation of polyhydroxybenzophenones as α-glucosidase inhibitors
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This experiment was designed to synthesize 18 kinds of polyhydroxybenzophenones by using Friedel-Crafts reaction, and to measure the inhibitory activity on α-glucosidase with p-nitrophenyl-β-D- galactopyranoside (PNPG) as a substrate. Here, acarbose (IC50a= a1674.75aaμmolaL-1) was used as the reference inhibitor. The results demonstrated that most of the target compounds had remarkable inhibitory activities on α-glucosidase. Among all these compounds, 2,4,4′,6-butahydroxydiphenylketone (11) was found to be the most potent α-glucosidase inhibitor with an IC50 value of 10.62aaμmolaL-1. In addition, we found these compounds were competitive inhibitors through the kinetic analysis. The results suggested that such compounds might be utilized for the development of new candidates for diabetes treatment. A series of polyhydroxybenzophenones was synthesized and evaluated as α-glucosidase inhibitors. Compound 11 was found to be the most potent inhibitor. Copyright
- Hu, Xuesen,Xiao, Yang,Wu, Jianlong,Ma, Lin
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experimental part
p. 71 - 77
(2011/09/21)
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- Synthesis and biological evaluation of polyhydroxy benzophenone as mushroom tyrosinase inhibitors
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A series of polyhydroxy benzophenone were synthesized and evaluated as mushroom tyrosinase inhibitors. The results demonstrated that most of the target compounds had remarkable inhibitory activities on mushroom tyrosinase. Among all these compounds, 2,3,4,3′,4′,5′-hexahydroxy-diphenylketone 10 was found to be the most potent tyrosinase inhibitor with IC50 value of 1.4 μM. In addition, the inhibition kinetics analyzed by Lineweaver-Burk plots revealed that such compounds were competitive inhibitors. These results suggested that such compounds might be utilized for the development of new candidate for treatment of dermatological disorders.
- Wu, Jianlong,Hu, Xuesen,Ma, Lin
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experimental part
p. 449 - 452
(2012/01/04)
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- DIPHENYLMETHANE COMPOUND
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Compounds having a diphenylmethane skeleton are superior in broad utility and stability, and are useful as a protecting reagent (anchor) of amino acid and/or peptide in the liquid phase synthesis and the like of a peptide having a C-terminal etc., which are of a carboxamide(-CONHR)-type, and in organic synthetic reaction methods (particularly peptide liquid phase synthetic methods), and may be contained in a kit for peptide liquid phase synthesis.
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- Synthesis of caged 2,3,3a,7a-tetrahydro-3,6-methanobenzofuran-7(6H)-ones: Evaluating the minimum structure for apoptosis induction by gambogic acid
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We have reported the discovery of gambogic acid (GA) as a potent apoptosis inducer and the identification of transferrin receptor as its molecular target. In order to understand the basic pharmacophore of GA for inducing apoptosis and to discover novel and simplified derivatives as potential anti-cancer agents, we explored the synthesis of caged 2,3,3a,7a-tetrahydro-3,6-methanobenzofuran-7(6H)-ones (4-oxatricyclo[4.3.1.0]decan-2-ones). Three types of 2,3,3a,7a-tetrahydro-3,6-methanobenzofuran-7(6H)-ones based on xanthone, 2-phenylchromene-4-one and benzophenone, were synthesized using a Claisen/Diels-Alder reaction cascade. All the reactions produced the targeted caged compound as well as its neo-isomer. The caged compounds based on xanthone and 2-phenylchromene-4-one were found to maintain the apoptosis inducing and cell growth inhibiting activity of GA, although with less potency. The caged compounds based on benzophenone were found to be inactive. Our study determined the minimum structure of GA for its apoptosis inducing activity, which could lead to the development of simple derivatives as potential anti-cancer drugs.
- Kuemmerle, Jared,Jiang, Songchun,Tseng, Ben,Kasibhatla, Shailaja,Drewe, John,Cai, Sui Xiong
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p. 4233 - 4241
(2008/09/21)
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- Selective ortho-cleavage of methoxymethyl- and 4-methoxybenzyl ethers
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Iodine in methanol has been found to be an effective catalyst system for the cleavage of alkoxymethyl ethers. This catalyst system is particularly useful for the selective removal of ortho-methoxymethyl- and ortho-(4-methoxybenzyl) ethers in the presence
- Keith, John M.
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p. 2739 - 2742
(2007/10/03)
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- Radiation-sensitive resin composition
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The radiation-sensitive resin composition, containing an alkali-soluble resin, comprises 1,1-bis(4-hydroxyphenol)-1-phenylethane, 1,1,1-tris(4-hydroxyphenyl)ethane or a compound selected from a polyhydroxy compound having the following formula: and quinonediazidesulfonates of the polyhydroxy compound, and the like. The radiation-sensitive resin composition is suitable for use as a positive type photoresist which has such excellent developability as to inhibit effectively the generation of scum in the formation of a photoresist pattern, has high sensitivity and is excellent in heat resistance and remained thickness ratio upon development.
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- Process of preparing light-sensitive naphthoquinonediazidesulfonic acid ester
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A light-sensitive mixture comprising a water-insoluble binder soluble in aqueous alkaline solutions, and the reaction product of a naphthoquinonediazidesulfonyl halide with a mixture composed of a low molecular weight compound having a definite structure and molecular size containing at least one phenolic hydroxyl group, and of a polymeric compound having recurring units, each of which contains at least one phenolic hydroxyl group. The mixture is useful in producing printing plates and photoresists and has the advantage that the naphthoquinonediazidesulfonic acid ester contained therein is non-explosive.
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