7506-46-9Relevant academic research and scientific papers
Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis
Bao, Xuefei,Chen, Guoliang,Du, Fangyu,Hammock, Bruce D.,Liu, Qiu,Liu, Zhongbo,Morisseau, Christophe,Sun, Wenjiao,Wang, Chao,Xiao, Wei,Yang, Hao,Zhang, Tan,Zhou, Jun
, (2021/07/06)
Sepsis, a systemic inflammatory response, caused by pathogenic factors including microorganisms, has high mortality and limited therapeutic approaches. Herein, a new soluble epoxide hydrolase (sEH) inhibitor series comprising a phenyl ring connected to a
Nickel-catalyzed reductive amidation of aryl-triazine ethers
Heravi, Majid M.,Panahi, Farhad,Iranpoor, Nasser
supporting information, p. 1992 - 1995 (2020/02/22)
The reaction of activated phenolic compounds, 2,4,6-triaryloxy-1,3,5-triazine (aryl-triazine ethers), with various isocyanates or carbodiimides in the presence of a nickel pre-catalyst resulted in the synthesis of aryl amides in good to excellent yields.
sEH inhibitor and preparation method and application thereof
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Paragraph 0234-0235; 0239-0240, (2020/07/28)
The invention provides an sEH inhibitor and a preparation method and application thereof, and relates to the technical field of endogenous active substance regulation and control. The sEH inhibitor provided by the invention has a structure as shown in a f
Immobilized Carbodiimide Assisted Flow Combinatorial Protocol to Facilitate Amide Coupling and Lactamization
Aldrich-Wright, Janice R.,Dankers, Christian,Gordon, Christopher P.,Harman, David G.,Nguyen, Thanh V.,Tadros, Joseph
supporting information, p. 255 - 267 (2020/06/05)
Through a screen of over one hundred and 30 permutations of reaction temperatures, solvents, carbodiimide resins, and carbodiimide molar equivalences, in the presence, absence, or combination of diisopropylamine and benzotriazole additives, a convenient and first reported carbodiimide polymer-assisted flow approach to effect amide coupling and lactamization was developed. The protocol entails injecting a single solution (1:9 dimethylformamide: dichloromethane) containing a carboxylic acid and an amine or linear peptide sequence into a continuous stream of dichloromethane. The protocol remained viable in the absence of base, did not require carboxylate preactivation which, and in concert with minimal workup requirements, enabled the isolation of products in high yields. Compared to the utilization of untethered carbodiimide reagents, the flow procedure was also observed to provide a degree of racemization safety.
Tert -Butyl nitrite promoted transamidation of secondary amides under metal and catalyst free conditions
Sureshbabu, Popuri,Azeez, Sadaf,Chaudhary, Priyanka,Kandasamy, Jeyakumar
, p. 845 - 850 (2019/01/30)
A mild and efficient method is demonstrated for the transamidation of secondary amides with various amines including primary, secondary, cyclic and acyclic amines in the presence of tert-butyl nitrite. The reaction proceeds through the N-nitrosamide intermediate and provides the transamidation products in good to excellent yields at room temperature. Moreover, the developed methodology does not require any catalyst or additives.
A Visible-Light-Driven, Metal-free Route to Aromatic Amides via Radical Arylation of Isonitriles
Malacarne, Marco,Protti, Stefano,Fagnoni, Maurizio
, p. 3826 - 3830 (2017/11/15)
The photochemical metal-free carboamidation of aryl radicals has been exploited for the preparation of aromatic amides, including hetero- and polyaromatic derivatives, under visible light irradiation of arylazo sulfones in the presence of isocyanides in aqueous acetonitrile. The process was useful for the smooth preparation of the antidepressant moclobemide. (Figure presented.).
Poly(methylhydrosiloxane) as a green reducing agent in organophosphorus-catalysed amide bond formation
Hamstra, Daan F. J.,Lenstra, Danny C.,Koenders, Tjeu J.,Rutjes, Floris P. J. T.,Mecinovi?, Jasmin
supporting information, p. 6426 - 6432 (2017/08/10)
Development of catalytic amide bond formation reactions has been the subject of the intensive investigations in the past decade. Herein we report an efficient organophosphorus-catalysed amidation reaction between unactivated carboxylic acids and amines. Poly(methylhydrosiloxane), a waste product of the silicon industry, is used as an inexpensive and green reducing agent for in situ reduction of phosphine oxide to phosphine. The reported method enables the synthesis of a wide range of secondary and tertiary amides in very good to excellent yields.
Nickel-Catalyzed Reductive Addition of Aryl/Benzyl Halides and Pseudohalides to Carbodiimides for the Synthesis of Amides
Panahi, Farhad,Jamedi, Fereshteh,Iranpoor, Nasser
, p. 780 - 788 (2017/01/18)
A Nickel-catalyzed reductive process is described for the direct amidation of benzyl and aryl halides using carbodiimides as the amidating agent. Moreover, aryl and benzyl C–O electrophiles such as triflate, acetate, tosylate, trityl ether, and pivalate were converted into amides using this method. The in-situ-generated Ni0acts as a catalyst for the reaction at room temperature for benzylic substrates, and 70 °C for aryl electrophiles. This new nickel-catalyzed reductive coupling protocol provides a general and operationally simple method for the synthesis of diverse amides using carbodiimides. Amides bearing bulky substituents can be synthesized by this strategy in high yield, which demonstrates its effectiveness in amide synthesis.
TfOH catalyzed One-Pot Schmidt–Ritter reaction for the synthesis of amides through N-acylimides
Singh, Garima,Dada, Ravikrishna,Yaragorla, Srinivasarao
supporting information, p. 4424 - 4427 (2016/09/13)
A One-Pot tandem Schmidt–Ritter process for the synthesis of amides has been developed using the super acid as catalyst. The in situ generated aryl/aliphatic nitriles from the reaction of aldehydes and sodium azide in the presence of TfOH and AcOH (Schmidt reaction) react with suitable alcohol (Ritter reaction) to give the amides. For the first time we observed that during the Schmidt process N-acylimides were generated along with nitriles, interestingly these N-acylimides also participated in the Ritter reaction.
The copper-catalyzed cross-coupling reactions of aryl diazonium salts and isocyanides
Li,Cao,Zhu,Zhang,Shi
, p. 668 - 671 (2016/06/01)
The copper-catalyzed cross-coupling reaction of aryl diazonium salts and isocyanides has been performed. This is a successful example of preparation of arylcarboxyamides with moderate to good yield under mild conditions.
