- Synthesis, biological evaluation and molecular dynamics studies of oxadiazine derivatives as potential anti-hepatotoxic agents
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Generally, herbal medicines having remarkable popularity for treating liver ailments, but they are still unacceptable because of the deprivation of herbal drug standardization. Therefore, there is a need for promising synthetic drugs to overcome the criti
- Ahmed, Bahar,Akbar, Saleem,Das, Subham,Iqubal, Ashif
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- Method for preparing diaryl ester compound through efficient catalysis of pyridine palladium
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The invention discloses a method for preparing a diaryl ester compound through efficient catalysis of pyridine palladium. The method is used for high-efficiency high-yield preparation of the diaryl ester compound under mild conditions by taking a phenol compound, an iodobenzene compound and carbon monoxide as raw materials, triethylamine as alkali and pyridine palladium as a catalyst. The method provided by the invention has the advantages of less usage amount of the palladium catalyst, high catalytic activity of the palladium catalyst, stability of the palladium catalyst to air, simple operation, short reaction time and high atom economy, opens up a low-cost, green and efficient way for preparation of diaryl ester compounds, and has broad application prospects.
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Paragraph 0016-0020; 0061-0065
(2020/12/31)
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- Nickel-Catalyzed Cross-Coupling of Aryl Redoxactive Esters with Aryl Zinc Reagents
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A nickel-catalyzed aryl-aroyloxyl C(sp2)-O radical cross-coupling reaction conducted using a redox active ester with aryl zinc reagent was developed. This method demonstrates a new disconnection approach for formation of aryl aryl esters. In the one-pot sequential process, the readily available aryl carboxylic acids can be converted into functionalized aryl aryl esters and heteroaryl esters. This protocol is amenable to the gram-scale synthesis. The present method has a wide substrate scope and high functional group tolerance.
- Shih, Bo-Hao,Basha, R. Sidick,Lee, Chin Fa
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p. 8862 - 8866
(2019/09/30)
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- Submillisecond organic synthesis: Outpacing Fries rearrangement through microfluidic rapid mixing
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In chemical synthesis, rapid intramolecular rearrangements often foil attempts at site-selective bimolecular functionalization.We developed a microfluidic technique that outpaces the very rapid anionic Fries rearrangement to chemoselectively functionalize iodophenyl carbamates at the ortho position. Central to the technique is a chip microreactor of our design, which can deliver a reaction time in the submillisecond range even at cryogenic temperatures.The microreactorwas applied to the synthesis of afesal, a bioactive molecule exhibiting anthelmintic activity, to demonstrate its potential for practical synthesis and production.
- Kim, Heejin,Min, Kyoung-Ik,Inoue, Keita,Im, Do Jin,Kim, Dong-Pyo,Yoshida, Jun-Ichi
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p. 691 - 694
(2016/05/19)
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- Solid-Phase Benzoylation of Phenols and Alcohols in Microwave Reactor: An Ecofriendly Protocol
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An efficient solid-phase benzoylation of phenols and alcohols was developed under microwave irradiation. A stoichiometric amount of benzoyl chloride was sufficient to carry out the reaction. This benzoylation features short reaction time, good yields, and easy workup procedures. Furthermore, the scope of the reaction was extended to prepare 3,5-dinitrobenzoyl derivatives of alcohols.
- Chakraborty, Suchandra,Saha, Ahana,Basu, Kaushik,Saha, Chandan
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supporting information
p. 2331 - 2343
(2015/10/12)
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- Montmorillonite K10 and KSF clays as acidic and green catalysts for effective esterification of phenols and alcohols under MWI
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Montmorillonite K-10 and KSF clays catalyze esterification of phenols and alcohols under microwave irradiation and solvent-free conditions in high yields within seconds.
- Marvi,Fekri,Takhti
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p. 1837 - 1840
(2015/01/09)
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- Metal-free synthesis of aryl esters by coupling aryl carboxylic acids and aryl boronic acids
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A facile synthesis of aryl esters is developed by coupling aryl carboxylic acids and aryl boronic acids in the presence of PhI(OAc)2 and carbonyl diimidazole. A wide range of functional groups were tolerant to the metal-free reaction condition that led to the desired products in good yields.
- Ruso, Jayaraman Sembian,Rajendiran, Nagappan,Kumaran, Rajendran Senthil
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supporting information
p. 2345 - 2347
(2014/05/06)
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- Ruthenium/NHC-catalyzed tandem benzylic oxidation/oxidative esterification of benzylic alcohols with phenols
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An efficient methodology to access benzoate derivatives via tandem benzylic oxidation/oxidative esterification of benzylic alcohols with phenols catalyzed by ruthenium/NHC was developed. This operationally simple one-pot process uses O2 as the clean oxidant, producing esters in good to excellent yields.
- Zhang, Di,Pan, Changduo
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experimental part
p. 41 - 45
(2012/06/18)
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- Palladium/NHC-catalyzed tandem benzylic oxidation/oxidative esterification of benzylic alcohols with phenols
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A palladium/NHC-catalyzed tandem benzylic oxidation/oxidative esterification of benzylic alcohols with phenols to access aryl benzoate derivatives is described. The procedure tolerates a series of functional groups, such as methoxy, nitro, cyano, chloro, fluoro and bromo groups. Thus, it represents a practically alternative method to access aryl benzoate derivatives.
- Luo, Fang,Pan, Changduo,Cheng, Jiang,Chen, Fan
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supporting information; experimental part
p. 5878 - 5882
(2011/09/12)
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- Palladium/NHC-catalyzed oxidative esterification of aldehydes with phenols
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A palladium-catalyzed oxidative esterification of aldehydes with phenols is described, using air as the clean oxidant. This reaction tolerates many functional groups, providing esters with yields ranging from moderate to excellent.
- Zhang, Manli,Zhang, Shouhui,Zhang, Guoying,Chen, Fan,Cheng, Jiang
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experimental part
p. 2480 - 2483
(2011/05/16)
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- Preparation of hydroxybenzophenones using silica-gel supported ferric chloride
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The synthesis of commercially important hydroxybenzophenones by condensing phenols with benzotrichloride has been reported. Benzoylation is catalyzed by silica supported ferric chloride under solvent-free conditions. Hydroxybenzophenones are isolated in low to moderate yields.
- Bendale, Pravin M.,Khadilkar, Bhushan M.
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p. 1738 - 1739
(2007/10/03)
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- LTA4 Hydrolase inhibitors
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The present invention provides compounds of the formula Ar1-Q-Ar2-Y-R-Z and pharmaceutically acceptable salts thereof wherein Ar1 and Ar2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as proriasis, ulcerative colitis, IBD and asthma.
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- Structure-activity relationship studies on 1-[2-(4- phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A4 (LTA4) hydrolase
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Leukotriene B4 (LTB4) is a pro-inflammatory mediator that has been implicated in the pathogenesis of a number of diseases including inflammatory bowel disease (IBD) and psoriasis. Since the action of LTA4 hydrolase is the rate-limiting step for LTB4 production, this enzyme represents an attractive pharmacological target for the suppression of LTB4 production. From an in- house screening program, SC-22716 (1, 1-[2-(4- phenylphenoxy)ethyl]pyrrolidine) was identified as a potent inhibitor of LTA4 hydrolase. Structure-activity relationship (SAR) studies around this structural class resulted in the identification of a number of novel, potent inhibitors of LTA4 hydrolase, several of which demonstrated good oral activity in a mouse ex vivo whole blood assay.
- Penning, Thomas D.,Chandrakumar, Nizal S.,Chen, Barbara B.,Chen, Helen Y.,Desai, Bipin N.,Djuric, Stevan W.,Docter, Stephen H.,Gasiecki, Alan F.,Haack, Richard A.,Miyashiro, Julie M.,Russell, Mark A.,Yu, Stella S.,Corley, David G.,Durley, Richard C.,Kilpatrick, Brian F.,Parnas, Barry L.,Askonas, Leslie J.,Gierse, James K.,Harding, Elizabeth I.,Highkin, Maureen K.,Kachur, James F.,Kim, Suzanne H.,Krivi, Gwen G.,Villani-Price, Doreen,Pyla, E. Yvonne,Smith, Walter G.,Ghoreishi-Haack, Nayereh S.
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p. 721 - 735
(2007/10/03)
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- PALLADIUM-CATALYZED OXIDATIVE COUPLING OF AROMATIC COMPOUNDS WITH OLEFINS USING t-BUTYL PERBENZOATE AS A HYDROGEN ACCEPTER
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Benzene and furans undergo oxidative coupling with olefins with an aid of t-butyl perbenzoate and a catalytic amount of Pd salts.The perbenzoate acts as a hydrogen accepter.In the absence of olefins, Pd catalyzed benzoxylation of aromatic compounds takes place.
- Tsuji, Jiro,Nagashima, Hideo
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p. 2699 - 2702
(2007/10/02)
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- The Kinetics and Mechanisms of Aromatic Halogen Substitution. Part 35. The Directive Effect of the Benzoyloxy-substituent
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The rates of chlorination of 4-acetamidophenyl benzoate, 1,3-bisbenzoyloxybenzene, and appropriate reference compounds by molecular chlorine in acetic acid at 25 deg C have been determined.By using the additivity principle, partial rate factors for chlorination directed by the benzoyloxy-group have thence been calculated, viz. fo-OCOPh 5.5, fm-OCOPh 0.059, fp-OCOPh 52.Comparison with analogous results obtained for the acetoxy-group allow estimates to be made of ?+ values for the benzyloxy-substituent.These values are used to discussed the course of halogenation of 2-benzoyloxynaphthalene.
- Brittain, Judith M.,Mare, Peter B. D. de la,Smith, Janet M.
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p. 1629 - 1632
(2007/10/02)
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