1143-72-2Relevant articles and documents
Synthesis method of 2,3,4-trihydroxybenzophenone
-
Paragraph 0031-, (2020/06/17)
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.
Synthesis and biological evaluation of polyhydroxy benzophenone as mushroom tyrosinase inhibitors
Wu, Jianlong,Hu, Xuesen,Ma, Lin
experimental part, p. 449 - 452 (2012/01/04)
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.
Synthesis of caged 2,3,3a,7a-tetrahydro-3,6-methanobenzofuran-7(6H)-ones: Evaluating the minimum structure for apoptosis induction by gambogic acid
Kuemmerle, Jared,Jiang, Songchun,Tseng, Ben,Kasibhatla, Shailaja,Drewe, John,Cai, Sui Xiong
, p. 4233 - 4241 (2008/09/21)
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.