- An unsymmetrical covalent organic polymer for catalytic amide synthesis
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Herein, we present the first report on the Covalent Organic Polymer (COP) directed non-classical synthesis of an amide bond. An economical route has been chosen for the synthesis of APC-COP using p-aminophenol and cyanuric chloride. APC-COP acts as a smart, valuable and sustainable catalyst for efficient access to the amide bond under mild conditions at room temperature in 30 min. APC-COP exhibits selectivity towards carboxylic acids over esters. The key features of this protocol involve the variety of parameters, viz. wider substrate scope, no use of additive and recyclability, which makes this approach highly desirable in gramscale synthesis. Moreover, we have shown the practical utility of the present method in the catalytic synthesis of paracetamol.
- Yadav, Deepika,Awasthi, Satish Kumar
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p. 179 - 186
(2019/12/28)
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- Reactions of difunctional electrophiles with functionalized aryllithium compounds: Remarkable chemoselectivity by flash chemistry
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Flash chemistry using flow microreactors enables highly chemoselective reactions of difunctional electrophiles with functionalized aryllithium compounds by virtue of extremely fast micromixing. The approach serves as a powerful method for protecting-group-free synthesis using organolithium compounds and opens a new possibility in the synthesis of polyfunctional organic molecules.
- Nagaki, Aiichiro,Imai, Keita,Ishiuchi, Satoshi,Yoshida, Jun-Ichi
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supporting information
p. 1914 - 1918
(2015/02/19)
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- Activity of diimidazoline amides against African trypanosomiasis
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We identified several diimidazoline mono- and diamides that were as potent as pentamidine against Trypanosoma brucei rhodesiense in vitro. All of these were also less cytotoxic than pentamidine, but none was as effective as the latter in a T. brucei rhode
- Dong, Yuxiang,Wang, Xiaofang,Cal, Monica,Kaiser, Marcel,Vennerstrom, Jonathan L.
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supporting information
p. 944 - 948
(2014/02/14)
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- Derivatives of N-phenylbenzamide with anti-ulcer and anti-allergy
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Derivatives of N-phenylbenzamide with general formula (1) in which R1 is a cyano, nitro, halogen, hydrozy, C1 -C4 alkyl methyl, methoxy or tetrazol-5-yl group, R2 is hydrogen, hydroxy, or methoxy, R3 is a tetrazol-5-yl group or hydrogen, R4 and R5 are hydrogen if R3 is tetrazolyl but are independently selected from the group consisting of carboxy, methoxycarbonyl, ethoxycarbonyl and carbamoyl if R3 is hydrogen, and R6 is hydrogen or methyl. The derivatives have an anti-ulcer and anti-allergy activity.
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- Antiallergic and cytoprotective activity of new N-phenylbenzamido acid derivatives
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A series of new N-phenylbenzamido acid derivatives was synthesized and evaluated for their ability to inhibit the IgE-mediated passive cutaneous anaphylaxis in the rat (PCA), as well as for their capacity to inhibit gastric mucosal damage induced by the oral administration of absolute alcohol in the rat. Some of these new derivatives exhibit potent antiallergic and cytoprotective activity, 20-80 times higher than that of the reference, disodium cromoglycate (DSCG). Structure-activity relationships are discussed. The antiallergic activity of one of the more potent compounds of this series, i.e. 4-(1H-tetrazol-5-yl)-N-[4-(1H-tetrazol-5-yl)phenyl]benzamide (compound 44, CR 2039) was further evaluated in vivo. This compound antagonizes the bronchoconstriction induced by aerosolized ovalbumin in both anesthetized and conscious IgE sensitized guinea pigs with ID50 of 3.7 mg/animal (tracheal insufflation) and 20 mg/kg (im). Further cytoprotective effects were evaluated in gastric ulcer models induced by the acute oral administration of hypertonic sodium chloride solution or by acetic acid and by the subchronic administration of glucose in fasted animals. In the models used experimentally CR 2039 is effective, whereas DSCG seems to be devoid of any protective activity. Such a potent antiallergic and mucosal protectant could provide a new potential agent in the therapy of atopic allergic diseases.
- Makovec,Peris,Revel,Giovanetti,Redaelli,Rovati
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p. 3633 - 3640
(2007/10/02)
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