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Synthesis, analgesic, anti-inflammatory, COX/5-LOX inhibition, ulcerogenic evaluation, and docking study of benzimidazole bearing indole and benzophenone analogs
Inflammation therapy is particularly focused on the development of safer non-steroidal anti-inflammatory drugs (NSAIDs), administered to control inflammation. It is typically considered that dual-inhibition of COX/5-LOX, which improves efficacy and has fewer side effects, is an effective technique for combating inflammation. In this perspective, the series of titled compounds (10a-j) were designed, synthesized, and characterized following with the anti-inflammatory, analgesic, and ulcerogenic evaluation. The investigation of the potentiality of the titled compounds (10a-j) displayed a high degree of anti-inflammatory activity. The compounds displaying potential analgesic activity were identified and validated further for evaluation of analgesic, anti-inflammatory activity, and subsequent ulcerogenic evaluation. In addition, the COX-1, COX-2, and 5-LOX analyses were carried out in vitro. Among (10a-j) series, compound 10c with para substitution of fluoro group on the benzoyl ring and two chloro groups at ortho position in phenyl ring of benzophenone was observed to have good inhibitory potency. Furthermore, the in silico docking study was performed by using AutoDock tools docking software.
Khamees, Hussien Ahmed,Khanum, Shaukath Ara,Nagesh, Khadri M. J.,Prashanth, T.
(2022/03/16)

Selective Oxidation of Alkylarenes to the Aromatic Ketones or Benzaldehydes with Water
Here a palladium-catalyzed oxidation method for converting alkylarenes into the aromatic ketones or benzaldehydes with water as the only oxygen donor is reported. This C-H bond oxidation functionalization does not require other oxidants and hydrogen accep
Du, Jihong,Duan, Baogen,Liu, Kun,Liu, Renhua,Yu, Feifei,Yuan, Yongkun,Zhang, Chenyang,Zhang, Jin
supporting information

(2022/02/09)

Aerobic Copper-Catalyzed Salicylaldehydic Cformyl?H Arylations with Arylboronic Acids
We report a challenging copper-catalyzed Cformyl?H arylation of salicylaldehydes with arylboronic acids that involves unique salicylaldehydic copper species that differ from reported salicylaldehydic rhodacycles and palladacycles. This protocol has high chemoselectivity for the Cformyl?H bond compared to the phenolic O?H bond involving copper catalysis under high reaction temperatures. This approach is compatible with a wide range of salicylaldehyde and arylboronic acid substrates, including estrone and carbazole derivatives, which leads to the corresponding arylation products. Mechanistic studies show that the 2-hydroxy group of the salicylaldehyde substrate triggers the formation of salicylaldehydic copper complexes through a CuI/CuII/CuIII catalytic cycle.
Xiao, Lin,Lang, Tao-Tao,Jiang, Ying,Zang, Zhong-Lin,Zhou, Cheng-He,Cai, Gui-Xin
supporting information
p. 3278 - 3283
(2021/02/01)

Preparation method of sun-screening agent 2-hydroxy-4-methoxy-5-sulfo benzophenone
The invention provides a preparation method of a sun-screening agent 2-hydroxy-4-methoxy-5-sulfo benzophenone. According to the method, SO3 is used as a sulfonating agent, the process conditions are mild, the reaction process is easy to control, the product selectivity is good, byproducts are few, and the purification process is simple and feasible. Compared with a traditional process, the production of waste acid is greatly reduced, the water content in the product is greatly reduced, acidic impurities are reduced to a great extent, the product quality is further improved, and the method is agreen and environment-friendly process and is beneficial to industrial production.
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Paragraph 0052-0053

(2021/02/06)

Preparation process of 2-hydroxy-4-methoxybenzophenone
The invention discloses a preparation process of 2-hydroxy-4-methoxybenzophenone, wherein the process comprises the steps: by using 2,4-dihydroxy benzophenone and halogenated methane as initial raw materials, generating 2-hydroxy-4-methoxybenzophenone under the actions of alkali liquor and a phase transfer catalyst. According to the method, cheap and easily available 2,4-dihydroxy benzophenone andhalogenated methane are used as starting raw materials, the preparation method is simple in process, green and environment-friendly, the product yield and purity are relatively high, and the method has a wide industrial application prospect.
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Paragraph 0035-0044

(2021/01/15)

Eco-friendly organocatalyst- And reagent-controlled selective construction of diverse and multifunctionalized 2-hydroxybenzophenone frameworks for potent UV-A/B filters by cascade benzannulation
The organocatalyst- and reagent-controlled highly selective synthesis of diversely functionalized novel 2-hydroxybenzophenone frameworks, such as 2-hydroxy-3′-formylbenzophenones, 7-(2′-hydroxybenzoyl)-2-naphthaldehydes, and 2-hydroxybenzophenones, under green conditions, for the development of potent UV-A/B filters is described. The organocatalyzed benzannulation reactions proceed individually via [3 + 3] cycloaddition for the synthesis of 2-hydroxy-3′-formylbenzophenones and [4 + 2] cycloaddition for 2-hydroxybenzophenones. With this methodology, an unprecedented double benzannulation allows one-pot construction of diverse 7-(2′-hydroxybenzoyl)-2-naphthaldehydes via [3 + 3 + 4] cycloaddition. This protocol features a broad substrate scope, high functional-group tolerance, and operational simplicity in an environmentally benign green solvent. The synthesized compounds are successfully utilized for further transformations and well characterized as potent UV-A/B filters.
Akhtar, Muhammad Saeed,Inductivo Tamargo, Ramuel John,Kim, Sung Hong,Lee, Yong Rok,Thombal, Raju S.,Yang, Won-Guen
supporting information
p. 4523 - 4531
(2020/08/10)

A Sunscreen-Based Photocage for Carbonyl Groups
Photolabile protecting groups (PPGs) have been exploited in a wide range of chemical and biological applications, due to their ability to provide spatial and temporal control over light-triggered activation. In this work, we explore the concept of a new photocage compound based on the commercial UVA/UVB filter oxybenzone (OB; 2-hydroxy-4-methoxybenzophenone) for photoprotection and controlled release of carbonyl groups. The point here is that oxybenzone not only acts as a mere PPG, but also provides, once released, UV photoprotection to the carbonyl derivative. This design points to a possible therapeutic approach to reduce the severe photoadverse effects of drugs containing a carbonyl chromophore.
Lineros-Rosa, Mauricio,Miranda, Miguel A.,Lhiaubet-Vallet, Virginie
p. 7205 - 7211
(2020/05/08)

Xantphos-ligated palladium dithiolates: An unprecedented and convenient catalyst for the carbonylative Suzuki–Miyaura cross-coupling reaction with high turnover number and turnover frequency
Xantphos- and dithiolate-ligated macrocyclic palladium complexes as an efficient and stable catalyst for the carbonylative Suzuki–Miyaura cross-coupling reaction have been synthesized. The catalysts were characterized by 1H-nuclear magnetic resonance (NMR), CHNS (carbon, hydrogen, nitrogen, and sulfur) analysis, melting point analysis, and 31P-NMR spectroscopy. Several sensitive functional groups (e.g., –NO2, –F, –Cl, –Br, –NH2, and –CN) on the aromatic ring were well tolerated in the carbonylative Suzuki–Miyaura coupling reaction. The present palladium complexes produce six times higher turnover number (TON) and five times higher turnover frequency (TOF) compared with conventional homogeneous palladium precursors. Maximum TONs in the range of 105 to 106 and TOF in the range of 104 to 105 could be generated by a very low amount of catalyst loading (10–5?mol%).
Gaikwad, Vinayak V.,Mane, Pravin A.,Dey, Sandip,Bhanage, Bhalchandra M.
(2019/11/19)

Deoxygenative Arylation of Carboxylic Acids by Aryl Migration
An unprecedented deoxygenative arylation of aromatic carboxylic acids has been achieved, allowing the construction of an enhanced library of unsymmetrical diaryl ketones. The synergistic photoredox catalysis and phosphoranyl radical chemistry allows for precise cleavage of a stronger C?O bond and formation of a weaker C?C bond by 1,5-aryl migration under mild reaction conditions. This new protocol is independent of substrate redox-potential, electronic, and substituent effects. It affords a general and promising access to 60 examples of synthetically versatile o-amino and o-hydroxy diaryl ketones under redox-neutral conditions. Furthermore, it also brings one concise route to the total synthesis of quinolone alkaloid, (±)-yaequinolone A2, and a viridicatin derivative in satisfying yields.
Ruzi, Rehanguli,Ma, Junyang,Yuan, Xiang-Ai,Wang, Wenliang,Wang, Shanshan,Zhang, Muliang,Dai, Jie,Xie, Jin,Zhu, Chengjian
p. 12724 - 12729
(2019/11/05)

Clean preparation method of 2-hydroxy-4-methoxy benzophenone
The invention discloses a clean preparation method of 2-hydroxy-4-methoxy benzophenone, and the clean preparation method is as follows: reacting 2,4-dihydroxybenzophenone and dimethyl carbonate as rawmaterials in the presence of a catalyst in a solvent for 4 to 6 hours at a controlled temperature of 100 to 200 DEG C in a medium pressure reaction kettle with a rectifying tower to obtain a crude reaction solution; filtering the crude reaction solution while the crude reaction solution is hot, respectively collecting solid substances and filtered mother liquor, cooling and crystallizing the filtered mother liquor, centrifuging, distilling and refining to obtain a 2-hydroxy-4-methoxy benzophenone fine product. According to the method, the green and environment-friendly dimethyl carbonate is adopted to replace highly toxic dimethyl sulfate for methylation synthesis reaction, carbon dioxide generated in the reaction is discharged through the use of a medium-pressure reaction device, and thesafety risk of the device is reduced. The conversion rate of the 2,4-dihydroxybenzophenone after the crude preparation reaction is over 99%, the content of main byproduct 2,4-dimethylbenzophenone isless than or equal to 5.0%, the finished product yield of the refined 2-hydroxy-4-methoxybenzophenone (BP-3) is more than or equal to 85%, and the purity meets USP quality requirements.
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Paragraph 0028-0047

(2019/10/01)

RhIII-Catalyzed Decarboxylative o-Acylation of Arenes Bearing an Oxidizing Directing Group
Here in we report, rhodium(III)-catalyzed decarboxylative acylation of arenes using α-oxocarboxylic acids as acyl surrogate. In this strategy, O–NHAc group act as an autocleavable oxidizing directing group (ODGauto), thus giving rise to ortho-acylated phenols in moderate to good yields. Mechanistic studies provided strong support for a kinetically relevant C–H bond activation. According to the best of our knowledge, this is the first report of Rhodium catalyzed decarboxylative acylation.
Bera, Suvankar,Chandrasekhar,Chatterjee, Satadru,Killi, Sunil Kumar,Sarkar, Debabrata,Banerji, Biswadip
p. 3877 - 3881
(2019/06/28)

Decarboxylation with Carbon Monoxide: The Direct Conversion of Carboxylic Acids into Potent Acid Triflate Electrophiles
We report a new strategy for the conversion of carboxylic acids into potent acid triflate electrophiles. The reaction involves oxidative carbonylation of carboxylic acids with I2 in the presence of AgOTf, and is postulated to proceed via acyl hypoiodites that react with CO to form acid triflates. Coupling this chemistry with subsequent trapping with arenes offers a mild, room temperature approach to generate ketones directly from broadly available carboxylic acids without the use of corrosive and reactive Lewis or Bronsted acid additives, and instead from compounds that are readily available, stable, and functional group compatible.
Kinney, R. Garrison,Arndtsen, Bruce A.
supporting information
p. 5085 - 5089
(2019/04/01)

Preparation method of ultraviolet absorbent UV-9
The invention provides a preparation method of an ultraviolet absorbent UV-9. The preparation method comprises following steps: step 1, water and methanol are added to a reaction kettle firstly, stirring is started, resorcinol is added, heating is performed, then benzotrichloride is dropwise added to the reaction kettle until the reaction is completed, mother liquor is subjected to centrifugal spin-drying, washing is performed until pH is neutral, and a UV-0 crude product is obtained; step 2, the UV-0 crude product, toluene and an acid-binding agent sodium carbonate are added to another reaction kettle, heating reflux is performed until no water drops appear, after cooling is performed, a catalyst PEG-400 is added, dimethyl sulfate is dropwise added, a mixture is heated after addition andsubjected to thermal insulation reaction until the components are reacted completely, water is added for washing, a product is left to stand for layering, organic phase is distilled under reduced pressure to remove an organic solvent methylbenzene, and a UV-9 crude product is obtained; step 3, the organic solvent is added to the UV-9 crude product for recrystallization, and a UV-9 finished productis obtained after centrifugation and drying. The problem of non-uniform color of the UV-9 product is solved, the product yield is increased, and the product cost is reduced.
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Paragraph 0024; 0028-0031; 0035-0038; 0042-0044

(2019/02/26)

Method for separating and purifying 5-chloro-2-hydroxy-4-methoxybenzophenone
The invention discloses a method for separating and purifying 5-chloro-2-hydroxy-4-methoxybenzophenone. The method includes the following steps: 1) recovering a solvent in the refining process of 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid to obtain a distillation concentrate and adding a sulfuric acid solution for reduction reaction with the temperature controlled at 80-130 DEG C; 2) conducting layering after reaction in the step 1), taking an organic phase in the lower layer, mixing with a mixed solvent composed of halogenated hydrocarbon and ester, cooling for crystallization, and distilling the remaining liquid substance to remove the mixed solvent to obtain a crude product of the 5-chloro-2-hydroxy-4-methoxybenzophenone; 3) adding the crude product of the 5-chloro-2-hydroxy-4-methoxybenzophenone into an alcohol solvent for recrystallization to obtain a pure product of the 5-chloro-2-hydroxy-4-methoxybenzophenone. In the preparation process of the 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid, active components of the refined mother liquor recovered concentrate is subjected to reduction, purification and purification, re-refining and purification to achieve separation andrecovery of target components.
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Paragraph 0039-0048

(2019/01/14)

COMPOUND AND COMPOSITION CONTAINING THE SAME, AND METHOD FOR MANUFACTURING DEVICE USING THE COMPOSITION
PROBLEM TO BE SOLVED: To provide a compound which efficiently absorbs extreme ultraviolet radiation (EUV) such as KrF excimer laser and ArF excimer laser or an electron beam, has low sensitivity to OoB, and has high contrast. SOLUTION: A compound is represented by formula (1) and formula (2). In formulae (1) and (2), R1a and R1a are each independently a first monovalent organic group containing a divalent hydrocarbon group selected from an alkylene group; a group bonded directly to sulfur atom (S+) is the divalent hydrocarbon group; R2 is a hydrogen atom, an alkyl group and the like; R3 to R6 are a hydrogen atom, a hydroxy group or a second monovalent organic group; X- is a monovalent anion; and R1a and R1b in Formula (1) or R1a and R1b in Formula (2) may be bonded to each other to form a ring. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
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Paragraph 0071-0073

(2017/09/14)

Carbonylative coupling of aryl tosylates/triflates with arylboronic acids under CO atmosphere
The carbonylative Suzuki-Miyaura reaction between aryl tosylates/triflates with arylboronic acid is herein reported, using base-free conditions and a balloon pressure of carbon monoxide. Under these conditions, unsymmetrical biaryl ketones were obtained in modest to excellent yields. This method was adapted to the synthesis of oxybenzone and ketoprofen in good yields under mild conditions.
Hao, Cheng Yi,Wang, Dan,Li, Ya Wei,Dong, Lin Lin,Jin, Ying,Zhang, Xiu Rong,Zhu, He Yun,Chang, Sheng
p. 86502 - 86509
(2016/09/23)

Bi (NO3)3·5H2O and cellulose mediated Cu-NPs - A highly efficient and novel catalytic system for aerobic oxidation of alcohols to carbonyls and synthesis of DFF from HMF
A highly efficient and versatile catalytic system for oxidation of primary and secondary aromatic alcohols to carbonyls has been developed. High efficiency, general synthetic applicability, broader functional group tolerance and versatility towards oxidation of both primary and secondary aromatic alcohols are the key features of this green and sustainable protocol. Selective oxidation of 5-hydroxymethyl furfural (HMF) to biofuel 2,5-diformylfuran (DFF) has been observed in excellent yields. Use of sustainable bio-polymer cellulose as a Cu-nanoparticle support makes the catalytic system environmentally benign.
Baruah, Diganta,Hussain, Farhaz L.,Suri, Mrinaly,Saikia, Ujwal Pratim,Sengupta, Pinaki,Dutta, Dipak Kumar,Konwar, Dilip
p. 9 - 12
(2016/01/20)

Synthesis of 2-acylphenol and flavene derivatives from the ruthenium-catalyzed oxidative c-h acylation of phenols with aldehydes
The cationic ruthenium hydride complex [(C6H6)(PCy3)(CO)RuH]+BF4- has been found to be an effective catalyst for the oxidative C-H coupling reaction of phenols with aldehydes to give 2-acylphenol compounds. The coupling of phenols with α,β-unsaturated aldehydes selectively gives the flavene derivatives. The catalytic method mediates direct oxidative C-H coupling of phenol and aldehyde substrates without using any metal oxidants or forming wasteful byproducts. A cationic ruthenium hydride complex catalyzes the oxidative C-H coupling of phenols with aldehydes to form 2-acylphenol and flavene derivatives.
Lee, Hanbin,Yi, Chae S.
p. 1899 - 1904
(2015/03/18)

Cosmetic compositions
Suggested is a cosmetic compositions comprising (a) a crosspolymer obtained from copolymerisation of at least two different polyols and at least one dicarboxylic acid and (b) at least one fragrance.
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(2014/07/08)

A composition for lightening skin and hair
Suggested is a composition comprising (a) sclareolide and (b1) at least one tyrosinase inhibitor; and/or (b2) at least one sun protection factor; and/or (b3) at least one anti-oxidants; and/or (b4) at least one anti-inflammatory agent; and/or (b5) at least one desquamating agent.
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(2014/10/28)

Palladacycles of thioethers catalyzing Suzuki-Miyaura C-C coupling: Generation and catalytic activity of nanoparticles
Tridentate thioether ligands, 2-HO-4-R-C6H3-(C 6H4)CHNH(CH2)3SPh [R = H (L1) or -OMe (L2)] react with Na2PdCl4, giving palladacycles [PdCl(C-,N,S)] (1: (C-,N,S) = L1-H; 2: (C-,N,S) = L2-H). The 1H and 13C{1H} NMR spectra of ligands and their palladacycles have been found to be characteristic. Complexes 1 and 2 have also been characterized with HR-MS. The crystal structure of 2 has been solved. The Pd-S bond length is 2.428(2) A, and palladium has a nearly square planar geometry. During the course of catalysis of Suzuki-Miyaura C-C coupling using 1 and 2 as catalysts, unexpected formation of Pd 16S7 nanoparticles (NPs) has been observed with both complexes. This is the first time that such an observation has been made with palladacycles of thioethers used in this coupling reaction. The efficiency of 2 in carrying out the coupling is significantly lower than that of 1. Complex 2 has an additional -OMe group in the ligand structure, and the size of Pd 16S7 NPs formed from this complex are larger (6 nm) than those obtained from 1 (2 nm).
Rao, Gyandshwar Kumar,Kumar, Arun,Kumar, Satyendra,Dupare, Umesh B.,Singh, Ajai K.
supporting information
p. 2452 - 2458
(2013/06/27)

Paramagnetic ruthenium(III) complexes bearing O,O chelating ligands: Synthesis, spectra, molecular structure and electron transfer properties
Paramagnetic Ru(III) complexes of the type [RuX2(EPh 3)2(L)] (where X = Cl or Br; E = P or As; L = monobasic bidentate benzophenone ligand) have been synthesized from the reaction of ruthenium(III) precursors, viz. [RuX3(EPh3)3] (where X = Cl, E = P; X = Cl or Br, E = As) or [RuBr3(PPh 3)2(CH3OH)] and substituted hydroxy benzophenones in a 1:1 molar ratio in benzene under reflux for 6 h. The hydroxy benzophenone ligands behave as monoanionic bidentate O,O donors and coordinate to ruthenium through the phenolate oxygen and ketonic oxygen atoms, generating a six-membered chelate ring. The compositions of the complexes have been established by analytical and spectral (FT-IR, UV-Vis, EPR) and X-ray crystallography methods. The single crystal structure of the complex [RuCl 2(PPh3)2(L1)] (1) has been determined by X-ray crystallography and indicates the presence of a distorted octahedral geometry in these complexes. The magnetic moment values of the complexes are in the range 1.75-1.89 μB, which reveals the presence of one unpaired electron in the metal ion. EPR spectra of liquid samples at liquid nitrogen temperature (LNT) show a rhombic distortion (g x ≠ gy ≠ gz) around the ruthenium ion. The complexes are redox active and display quasi-reversible oxidation and quasi-reversible reduction waves versus Ag/AgCl.
Raja, Nandhagopal,Ramesh, Rengan,Liu, Yu
experimental part
p. 196 - 201
(2012/03/11)

Synthesis of fluorenone derivatives through Pd-catalyzed dehydrogenative cyclization
Palladium-catalyzed dual C-H functionalization of benzophenones to form fluorenones by oxidative dehydrogenative cyclization is reported. This method provides a concise and effective route toward the synthesis of fluorenone derivatives, which shows outstanding functional group compatibility.
Li, Hu,Zhu, Ru-Yi,Shi, Wen-Juan,He, Ke-Han,Shi, Zhang-Jie
supporting information
p. 4850 - 4853,4
(2012/12/12)

Modular synthesis of polyphenolic benzofurans, and application in the total synthesis of malibatol A and shoreaphenol
A modular strategy for the synthesis of hexacyclic dimeric resveratrol polyphenolic benzofurans is reported. The developed synthetic technology was applied to the total synthesis of malibatol A, shoreaphenol, and other biologically relevant polyphenols.
Chen, David Y.-K.,Kang, Qiang,Wu, T. Robert
experimental part
p. 5909 - 5927
(2010/11/05)

AHR MEDIATORS
The invention relates to a method for finding and assessing agonists [and] antagonists of the aryl hydrocarbon receptor (Ah receptor; AhR), to the agonists and antagonists themselves and to uses thereof
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(2009/02/11)

BENZOFURAN AND BENZOTHIOPHENE-2-CARBOXYLIC ACID AMIDE DERIVATIVES
The present invention relates to compounds of formula I wherein X, A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
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Page/Page column 23

(2009/02/11)

Substituted hexahydro-1,4-diazepin-5-ones and compositions stabilized therewith
The instant invention pertains to white, dyed, dipped, unscented and/or scented candle wax which is effectively stabilized against discoloration and fading by the incorporation therein of a substituted hexahydro-1,4-diazepin-5-ones in combination with a UV absorber and/or an antioxidant. Additionally, some novel substituted hexahydro-1,4-diazepin-5-one compounds are described.
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(2008/06/13)

Benzoic acid ester compounds, compositions, uses and methods related thereto
Benzoic acid ester compounds of formula (I): wherein R and R1-R5 are as defined in the description, methods for producing them and use thereof in cosmetic, pharmaceutical, personal care and industrial preparations as sunscreens based on photochemical precursor properties of ultraviolet absorbers.
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Page/Page column 17; 38

(2010/11/23)

SUNSCREEN COMPOSITIONS
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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(2008/06/13)

Novel indanylidene compounds
Novel indanylidene compounds can be used as UV-A filters in cosmetic compositions for protecting skin and hair and for technical applications.
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(2008/06/13)

Method of purifying arylphenones
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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(2008/06/13)

Phosphites and their production and use
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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(2008/06/13)

Piperidine compound, a process for producing the same and a stabilizer using the same
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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(2008/06/13)

BeCl2 as a new highly selective reagent for dealkylation of aryl-methyl ethers
An efficient and simple method is introduced for the selective removal of methyl group from poly aryl-methyl ethers, in some important derivatives of benzophenones, xanthones, anthraquinones, aryl esters, benzamides and nitroanisoles with BeCl2.
Sharghi, Hashem,Tamaddon, Fatemeh
p. 13623 - 13640
(2007/10/03)

Studies on uricosuric diuretics. II. Substituted 7,8-dihydrofuro[2,3-g]-1,2-benzisoxazole-7-carboxylic acids and 7,8-dihydrofuro[2,3-g]benzoxazole-7-carboxylic acids
A series of substituted 7,8-dihydrofuro[2,3-g]-1,2-benzisoxazole-7-carboxylic acids and 7,8-dihydrofuro[2,3-g]benzoxazole-7-carboxylic acids were synthesized and evaluated for uricosuric and diuretic activities in rats. Many of the benzisoxazole derivatives showed uricosuric and only weak diuretic activities, whereas the benzoxazoles exhibited potent diuretic activities with little affecting urate excretion. Among these compounds, 5-chloro-7,8-dihydro-3-phenylfuro[2,3-g]-1,2-benzisoxazole-7-carboxylic acid (AA-193) was found to be a potent uricosuric agent without diuretic activity and was selected for further development.
Sato,Dan,Onuma,Tanaka,Aoki,Koga
p. 1760 - 1772
(2007/10/02)

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
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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(2008/06/13)

A Complex Induced Proximity Effect in the Anionic Fries Rearrangement of o-Iodophenyl Benzoates: Synthesis of Dihydro-O-methylsterigmatocystin and Other Xanthones
The success of an anionic Fries rearrangement, used to synthesise dihydro-O-methylsterigmatocystin and other xanthones, is dependent on the presence of a remote methoxyl substituent.
Horne, Stephen,Rodrigo, Russell
p. 4520 - 4522
(2007/10/02)

Cosmetic screening composition containing a UV screen in combination with a polymer obtained by block polymerization in emulsion and its use for the protection of the human epidermis against ultraviolet radiations
Cosmetic screening composition containing a UV screen in combination with a polymer obtained by block polymerization in emulsion and its use for the protection of the human epidermis against ultraviolet radiations.
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(2008/06/13)

BORON TRICHLORIDE CATALYZED ORTHO CARBONYLATION OF PHENOLS: SYNTHESIS OF 2-HYDROXY-ARYL-CARBOXYAMIDES AND -KETONES.
In the presence of equimolar quantity of BCl3, phenols 1 react with isocyanates and acyl chlorides to give, usually with good-excellent yields, 2-hydroxy-aryl-carboxy-amides 2 and 2-hydroxy-aryl-ketones 3 respectively.A distinctive behaviour of BCl3 in comparison with other Lewis acids is observed.
Piccolo, Oreste,Filippini, Lucio,Tinucci, Laura,Valoti, Ermanno,Citterio, Attilio
p. 885 - 892
(2007/10/02)

PHOTOCHEMISTRY OF LATIFOLIN AND SOME RELATED COMPOUNDS
Latifolin (1), the major constituent of D. latifolia gave trans 1-(2,4-dimethoxy-3-hydroxyphenyl)-2-(2-hydroxyphenyl) cyclopropane as the sole photo di-?-methane rearrangement product.In contrast, its simpler analogues, 3-(2,4,5-trimethoxyphenyl)-3-phenyl prop-1-ene (3) and 3-(2,4-dimethoxyphenyl)-3-phenyl prop-1-ene (4), gave 1:1 mixture of cis and trans cyclopropanes.Dye-sensitized photooxidation of latifolin (1) and dihydrolatifolin (16) gave novel xanthan derivatives (15) and (17) involving a crucial step of photooxidative demethylation followed by cyclisation.Similar reaction of the closely related propane 19 gave, interestingly the benzofuran 20.The propene 22, lacking free hydroxyl or double bond, gave only the quinone 23 indicating that quinones are intermediates in the above oxidations.The allyl alcohol 24, having similar feature, undergoes oxidation to the corresponding aldehyde 26 and the benzophenone 28 but not to a quinone.
Walia, S.,Kulshrestha, S.K.,Mukerjee, S.K.
p. 4817 - 4826
(2007/10/02)

Method of treating inflammation
A method of treating inflammation and inhibiting prostaglandin synthesis employing 2-hydroxybenzophenone and substituted 2-hydroxybenzophenones.
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(2008/06/13)

High molecular weight piperidine derivatives as UV stabilizers
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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(2008/06/13)

Process for preparing a 5,5'-methylenebis(2-hydroxy-4-alkoxybenzophenone)
A novel process is provided for preparing 5,5'-methylenebis(2-hydroxy-4-alkoxybenzophenone), comprising forming a novel 2-hydroxy-4-alkoxy-5-aminomethylbenzophenone by a reaction of a 2-hydroxy-4-alkoxybenzophenone with an amine and formaldehyde, and causing the 2-hydroxy-4-alkoxy-5-aminomethylbenzophenone to react with a 2-hydroxy-4-alkoxybenzophenone or to dimerize. Both the aminomethylhydroxyalkoxybenzophenone and the methylenebis (2-hydroxy-4-alkoxybenzophenone) which are prepared according to this invention are useful to prevent photo-degradation of organic materials, particularly as light stabilizers for synthetic resins.
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(2008/06/13)

1-Aza-4-thiacyclohexane-4,4-dioxide derivatives
New 1-aza-4-thiacyclohexane-4,4-dioxide derivatives are used alone or in combination with other stabilizers for stabilizing organic materials. The new compounds are prepared by reacting substituted diallylsulfides with ammonia, amines or hydrazines.
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(2008/06/13)