- Method for catalytically synthesizing ultraviolet light absorber BP-2
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The invention discloses a method for catalytically synthesizing an ultraviolet light absorber BP-2. The method comprises the following steps: (1) adding a halogenated hydrocarbon solvent and a composite catalyst into a reactor, uniform stirring and mixing, heating to 90-120 DEG C, adding 2,4-dihydroxybenzoic acid and m-diphenol into the mixture, carrying out stirring dissolving, carrying out a thermal insulation reaction for 2-3 h, after the reaction is finished, filtering while hot to recover the catalyst graphite, adding a proper amount of water into the filtrate, heating to 90-100 DEG C, completely stirring and dissolving, standing for layering, distilling an organic layer to recover a solvent, cooling a water layer to 10-20 DEG C, separating out a large amount of red crystals, carryingout suction filtration, and washing with water to obtain a crude product; and (2) dissolving the crude product with a proper amount of hot water, adding activated carbon to decolorize, boiling for 30-60 minutes, filtering while hot, cooling and crystallizing to obtain a light yellow green crystal ultraviolet light absorber BP-2 product with the melting point of 199-200 DEG C and the purity of more than or equal to 99.8%. The method is high in synthesis yield, simple in production process, high in product purity, low in cost and suitable for industrial production.
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Paragraph 0020; 0030-0033; 0038-0049
(2020/11/23)
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- Synthetic method of ultraviolet ray absorber BP-2
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The invention discloses a synthetic method of an ultraviolet ray absorber BP-2. The method mainly comprises the following steps: 1, carrying out an esterification reaction: adding resorcinol and chloroform to a reaction kettle, adding acetyl chloride in a dropwise manner after dissolving, and reacting for 2-2.5h to obtain diphenol acetate; 2, carrying out an acylation reaction: adding the esterification product diphenol acetate, dichloroethanes, N,N-dimethyl formamide and anhydrous aluminum trichloride to the reaction kettle, slowly adding solid phosgene in a dropwise manner, reacting, distilling the above obtained product to recover a solvent, and cooling solid residues in the kettle to room temperature; and 3, carrying out a hydrolysis reaction: dissolving the solid residues in the kettle in 10% diluted hydrochloric acid, carrying out a heating hydrolysis reaction, cooling the obtained product, standing the cooled product to precipitate a solid, carrying out pumping filtration, washing the obtained solid with water to obtain a crude product, and purifying the crude product to obtain the BP-2. The method has the advantages of simple process, mild conditions, low production cost, and suitableness for industrial production.
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- Synthesis, SAR and biological evaluation of natural and non-natural hydroxylated and prenylated xanthones as antitumor agents
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In order to explore the detailed structure-activity relationship (SAR) around xanthone scaffold bearing hydroxyl and prenyl moieties, twenty-nine natural and non-natural hydroxylated and prenylated xanthones have been synthesized and evaluated for their in vitro anti-proliferative activities against five human cancer cell lines, including HepG2 (hepatocelluar carcinoma), HCT-116 (colon carcinoma), A549 (lung carcinoma), BGC823 (gastric carcinoma) and MDAMB- 231 (breast carcinoma). The SAR analysis revealed that the anti-proliferative activity of the xanthones is substantially influenced by the position and number of attached hydroxyl and prenyl groups, and the presence of hydroxyl group ortho to the carbonyl function of xanthone scaffold contributes significantly to their cytotoxicity. The new prenylated xanthone 20 with a relatively simple structure, namely 1,3,8-trihydroxy-2-prenylxanthone, was found to exhibit potent antitumor activities comparable to mangostin against all the five cancer cell lines. Further mechanistic studies suggested that compound 20 induces apoptosis and causes cell cycle arrest at S phase in HepG2 cells. These results have highlighted compound 20 as a new potential lead candidate for future development of novel potent broad-spectrum antitumor agents.
- Zhang, Xiaojin,Li, Xiang,Tao, Lei,Gao, Yuan,Gong, Dandan,Xi, Meiyang,Xu, Xiaoli,Guo, Qinglong,You, Qidong,Ye, Suofu,Zhang, Yu,Meng, Huyan,Zhang, Mingqian,Gao, Wenlei
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p. 1012 - 1025,14
(2012/12/12)
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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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- Body-care and household products and compositions comprising specific sulfur-containing compounds
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Disclosed are stabilized body care products, household products, textiles and fabrics which comprise specific sulfur containing compounds. Dyed products and articles are effectively stabilized against color degradation. The products are for example skin-care products, hair-care products, dentifrices, cosmetics, laundry detergents and fabric softeners, non-detergent based fabric care products, household cleaners and textile-care products.
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- SUNSCREEN COMPOSITIONS
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The present invention relates to improved sunscreen compositions, more preferably to improved sunscreen compositions containing at least one sunscreening agent (sunscreen) and a silicone-polyamide copolymer.
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- Preparation of hydroxylated benzophenones
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Hydroxylated benzophenonens are prepared from completely or partially methylated hydroxybenzophenones by reacting these methyl ethers with AlCl3 and subsequently hydrolyzing with water, the reaction being carried out in the presence of one or more compounds from the class of ureas or carboxamides.
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- Method of purifying arylphenones
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Hydroxy and alkyloxy benzophenones, also known as arylphenones, are efficiently and economically purified by contacting them with inorganic phosphorous compounds in the presence of a non-polar solvent. Best results are obtained when the arylphenone is then treated with an activated carbon and/or activated clay.
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- Phosphites and their production and use
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Phosphites represented by the general formula (I): STR1 wherein R1, R2, R4 and R5 independently represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a cycloalkyl group having 5 to 8 carbon atoms, an alkylcycloalkyl group having 6 to 12 carbon atoms, an aralkyl group having 7 to 12 carbon atoms or a phenyl group; R3 and R6 independently represent a hydrogen atom or an alkyl group having 1 to 8 carbon atoms; X1 is a dihydric alcohol residue, wherein HO--X1 --OH defines the corresponding dihydric alcohol from which residue X1, is obtained; and X2 is a direct bond or an alkylene group having 1 to 8 carbon atoms; and the phosphites are useful as stabilizers for organic materials.
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- Piperidine compound, a process for producing the same and a stabilizer using the same
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2-Methyl-3-(2,2,6,6-tetramethyl-4-piperidylamino)-N-(2,2,6,6-tetramethyl-4-piperidyl)-propionamide represented by the following formula, a process for producing the same and a stabilized organic material composition containing the same wherein the piperidine compound imparts excellent properties, such as light stability or thermal stability to the organic materials. STR1
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- Method for dyeing keratinous fibres using a monohydroxyindole or dihydroxyindole and a non-oxidizing aromatic carbonyl derivative and dyeing agent
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The present invention relates to a method for dyeing keratinous fibers, characterized in that the following are applied to the fibers: a) a composition (A) containing, in a medium appropriate for dyeing, at least one monohydroxyindole or dihydroxyindole, this application being preceded or followed by the application of b) a composition (B) containing, in a medium appropriate for dyeing, at least one aromatic carbonyl derivative chosen from hydroxyacetophenones, hydroxybenzophenones, 2-hydroxy-1,4-benzoquinones, hydroxy-1,4-naphthoquinones,amino-1,4-naphthoquinones,hydroxy-9,10-anthraquinones and amino-9,10-anthraquinones. It also relates to the dyeing agents for carrying it out.
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- Light-stable screening cosmetic composition containing bixin combined with a lipid-soluble UV filter and its use for protecting the human epidermis against ultra-violet radiation
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The invention relates to a light-stable cosmetic composition for protecting the human epidermis against UV radiation, containing at least 0.0025% by weight of bixin combined with at least 1% by weight of one or more lipid-soluble agents screening UV radiation, chosen from 3-benzylidene-dl-camphor, its derivatives and benzophenone derivatives, in a cosmetically acceptable vehicle comprising at least one fatty phase. The bixin takes the form of an oily extract of annatto containing at least 0.1% by weight of bixin.
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- High molecular weight piperidine derivatives as UV stabilizers
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Substituted high molecular weight hindered spiropiperidine compounds and polymer compositions stabilized by these compounds. The spiropiperidine compounds are prepared by reacting hindered 4-piperidinone hydrochloride with an activated benzene, such as resorcinol, in an acid medium.
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