- Studies towards the design and synthesis of novel 1,5-diaryl-1h-imidazole-4-carboxylic acids and 1,5-diaryl-1h-imidazole-4-carbohydrazides as host ledgf/p75 and hiv-1 integrase interaction inhibitors
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Two targeted sets of novel 1,5-diaryl-1H-imidazole-4-carboxylic acids 10 and carbohy-drazides 11 were designed and synthesized from their corresponding ester intermediates 17, which were prepared via cycloaddition of ethyl isocyanoacetate 16 and diarylimi
- Bode, Moira L.,Fish, Muhammad Q.,Mabel Coyanis, E.,Rashamuse, Thompho J.
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- Green synthetic method of N-arylamides using recyclable cheap metal catalyst
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Magnetically separable and reusable Fe/Cu oxide (Fe3O4-Cu2O) nanoparticles were employed as an efficient catalyst for the arylation of benzamide, which was carried out with a range of both arylboronic acid and benzamide to afford N-arylamide in good to excellent yield.
- Wang, Xingyang,Liu, Jianhui,An, Guanghui
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supporting information
(2020/10/05)
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- Carbon-Carbon Bond Formation of Trifluoroacetyl Amides with Grignard Reagents via C(O)-CF3 Bond Cleavage
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The reaction of trifluoroacetyl amides with Grignard reagent for the substitution of CF3 group with various alkyl or aryl groups is described. A variety of aryl, quinolin-8-yl, and (hetero)alkyl functional groups as well as F, Cl, and Br atoms are well tolerated. These moisture-stable and easily available trifluoroacetyl amides can be conveniently obtained and used as new versatile precursors for isocyanates. The control experiments show that the reaction proceeds via an isocyanate intermediate and/or alkoxide/amide dual anionic intermediate.
- Zhu, Longzhi,Le, Liyuan,Yan, Mingpan,Au, Chak-Tong,Qiu, Renhua,Kambe, Nobuaki
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p. 5635 - 5644
(2019/05/10)
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- Carbon-Carbon Bond Formation of Trifluoroacetyl Amides with Grignard Reagents via C(O)-CF3 Bond Cleavage
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The reaction of trifluoroacetyl amides with Grignard reagent for the substitution of CF3 group with various alkyl or aryl groups is described. A variety of aryl, quinolin-8-yl, and (hetero)alkyl functional groups as well as F, Cl, and Br atoms are well tolerated. These moisture-stable and easily available trifluoroacetyl amides can be conveniently obtained and used as new versatile precursors for isocyanates. The control experiments show that the reaction proceeds via an isocyanate intermediate and/or alkoxide/amide dual anionic intermediate.
- Zhu, Longzhi,Le, Liyuan,Yan, Mingpan,Au, Chak-Tong,Qiu, Renhua,Kambe, Nobuaki
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- Mn(III)-mediated radical cascade reaction of boronic acids with isocyanides: Synthesis of diimide derivatives
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A manganese(III)-promoted oxidative radical cascade reaction of easily accessible arylboronic acids with isocyanides to construct diimide derivatives was studied. This protocol provides a new way to synthesis of acetyl diimide derivatives. New C–C, C–N and C[dbnd]O bonds were formed in one step.
- Wang, Fei,Wei, Tian-Qi,Xu, Pei,Wang, Shun-Yi,Ji, Shun-Jun
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supporting information
p. 379 - 382
(2018/09/11)
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- Preparation method of amide compounds
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The invention discloses a novel preparation method of amide compounds. According to the preparation method, perfluoroalkyl amide is taken as the raw material, a transition metal catalyst is adopted, perfluoroalkyl amide carries out reactions for a while in an organic aprotic solvent at a certain temperature, amide compounds can be obtained high selectively, and the yield is high. The preparation method has the advantages of low cost, high yield, and simple and convenient operation, and can be possibly applied to industrial production.
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Paragraph 0029-0030
(2018/09/28)
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- Chemoselective Synthesis of N-arylbenzamides and Benzoyloxyacetanilides from Aryl Isocyanides: Styrene as Aryl and Arylcarboxymethylene Source
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Styrenes serve as unique aryl or arylcarboxymethylene source towards aryl isocyanides in the presence of Cu(II)/TBHP, and yield N-arylbenzamides or benzoyloxyacetanilides respectively. The chemoselectivity of the reaction is controlled by the nature of the substituents present on styrene ring. Whereas styrenes substituted with electron-releasing alkyl and alkoxy groups yield N-arylbenzamides, unsubstituted styrene and those with electron-withdrawing substituents furnish benzoyloxyacetanilides as the major product. With benzylamines as the substrate, N-arylbenzamides are formed exclusively as they act only as an aryl donor. TBHP serves as a promoter and oxygen source. Both the pathways are believed to proceed through an initial oxidative C?C bond cleavage of styrene. (Figure presented.).
- Sharma, Poonam,Jain, Nidhi
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supporting information
p. 1932 - 1937
(2018/03/27)
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- Synthesis of Secondary Amides through the Palladium(II)-Catalyzed Aminocarbonylation of Arylboronic Acids with Amines or Hydrazines and Carbon Dioxide
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A new Pd-catalyzed aminocarbonylation of arylboronic acids with amines or phenylhydrazines has been developed. Various secondary amides were produced from readily available substrates and cheap common metal catalysts in a CO atmosphere (balloon). Remarkably, we presents the first example of aminocarbonylations between arylboronic acids and phenylhydrazines.
- Zhang, Jin,Ma, Yuqiang,Ma, Yangmin
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supporting information
p. 1720 - 1725
(2018/04/24)
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- Potassium Carbonate Promoted C-N Coupling Reaction between Benzamides and Aryl Iodides
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A practical and efficient method for N-arylation of benz-amides promoted by potassium carbonate in the presence of DMEDA was developed. The reaction was carried out without addition of any transition-metal catalyst to afford a variety of N-arylated products in moderate to good yields (up to 97%).
- Huang, Fei,Wu, San,Hu, Weiye,Zhang, Songlin
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supporting information
p. 1090 - 1096
(2017/11/29)
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- Copper(I) iodide–catalyzed amidation of phenylboronic acids/aryl bromides using 4-dimethylaminopyridine as ligand
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An efficient one-pot synthesis of N-arylbenzamide is described via reaction of phenylboronic acid/aryl bromide with benzamide in the presence of CuI (5?mol%) as catalyst, 4-dimethylaminopyridine (20?mol%) as the ligand, and Cs2CO3(2?mmol) as the base. This protocol was applied to synthesize a small library of N-arylbenzamide in high yields.
- Alapati, Mohan Lakshmi Punna Rao,Abburu, Sridhar Rao,Mutyala, Krishnaji Rao,Mukkamala, Saratchandra Babu
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supporting information
p. 1242 - 1248
(2016/08/06)
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- Synthesis of polysubstituted-1,2,4-triazoles
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A new series of substituted 1,2,4-triazole derivatives have been synthesized using substituted imido derivatives and isonicotinyl hydrazine (or 4-nitrobenzoylhydrazine) as the key intermediates. These compounds include different donor or acceptor substitu
- Liu, Guiyan,Wu, Xueli,Shi, Xuefang
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- Facile AlCl3-promoted catalytic beckmann rearrangement of ketoximes
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Aluminum chloride, an inexpensive and commercially available Lewis acid traditionally employed for Beckmann rearrangement with stoichiometric amounts, has been now found to smoothly promote the Beckmann rearrangement of various ketoximes to the corresponding amides (up to 99% of yield) with 10mol% catalyst loading in anhydrous acetonitrile under reflux temperature.
- Liu, Li-Feng,Liu, Hua,Pi, Hong-Jun,Yang, Shuo,Yao, Min,Du, Wenting,Deng, Wei-Ping
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experimental part
p. 553 - 560
(2011/04/22)
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- A mild and highly efficient catalyst for Beckmann rearrangement, BF 3·OEt2
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BF3·OEt2 (Boron trifluoride etherate), an inexpensive and commercially easily available Lewis acid stoichiometrically employed for Beckamann rearrangement in general, was now found to efficiently catalyze Beckmann rearrangement of ketoximes into their corresponding amides (up to 99% yield) in anhydrous acetonitrile under reflux temperature.
- An, Na,Pi, Hongjun,Liu, Lifeng,Du, Wenting,Deng, Weiping
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experimental part
p. 947 - 950
(2012/01/05)
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- Cyclopentadienyl-free rare-earth metal amides [{(CH2SiMe 2){(2,6iPr2C6H3)N} 2}Ln{N(SiMe3)2}(THF)] as highly efficient versatile catalysts for C-C and C-N bond formation
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Efficient methods have been developed for the direct synthesis of amides from aldehydes and a straightforward route to propiolamidines using cyclopentadienyl-free rare-earth metal amides [{(CH2SiMe 2){(2,6-iPr2C6H3)N} 2}Ln{N(SiMe3)2}(THF)] [Ln = Yb (1), Y (2), Dy (3), Sm (4), Nd (5)] as versatile catalysts, The results indicate that in the direct synthesis of amides from aldehydes the catalysts have the activity order 2>1~3~4~5. These methods have the advantage of easy preparation of the catalysts, low catalyst loading, high conversion of substrates to products, mild reaction conditions, and compatibility with a wide range of substrates.
- Wu, Yunjun,Wang, Shaowu,Zhang, Lijun,Yang, Gaosheng,Zhu, Xiancui,Zhou, Zhihong,Zhu, Hong,Wu, Shihong
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supporting information; experimental part
p. 326 - 332
(2010/04/06)
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- Unexpected results from the re-investigation of the Beckmann rearrangement of ketoximes into amides by using TsCl
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TsCl (p-toluenesulfonyl chloride), a commercially available organosulfonyl chloride, has been widely used as a stoichiometric dehydrogenation reagent in the transformation of ketoximes into corresponding amides via the Beckmann rearrangement. It has been now found to catalyze the Beckmann rearrangement with high catalytic efficiency, converting a wide range of ketoximes into their corresponding amides under mild condition with good to excellent yields (up to 99% of yield with 1-5 mol % of catalyst loading).
- Pi, Hong-Jun,Dong, Jin-Dong,An, Na,Du, Wenting,Deng, Wei-Ping
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experimental part
p. 7790 - 7793
(2010/01/06)
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- Highly efficient synthesis of fused bicyclic 2,3-diaryl-pyrimidin-4(3H)-ones via Lewis acid assisted cyclization reaction
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An expedient one-pot synthesis of fused bicyclic 2,3-diaryl-pyrimidin-4(3H)-ones from three readily available components is described. The key step is a Lewis acid assisted cyclization reaction.
- Yang, Kunyong,He, Xiaohui,Choi, Ha-soon,Wang, Zhicheng,Woodmansee, David H.,Liu, Hong
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p. 1725 - 1728
(2008/09/17)
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- Organic Phosphorus Compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as Potent Calcium Antagonistic Vasodilator
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A series of 4-(benzothiazol-2-yl)benzylphosphonic acid dialkyl ester were synthesized and evaluated for coronary vasodilatory activity by Langendorff's method in the isolated guinea pig heart. Many of the phosphonic acid dialkyl esters exhibited vasodilat
- Yoshino, Kohichiro,Kohno, Toshihiko,Uno, Toshio,Morita, Tominori,Tsukamoto, Goro
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p. 820 - 825
(2007/10/02)
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- A Novel Synthesis of 3-Aryl-1,2,4-benzotriazines via N-Phenylsulfonyl-N''-arylbenzamidrazones
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3-Aryl-1,2,4-benzotriazines were obtained in good yields by the mercury(II) oxide-oxidation of N-phenylsulfonyl-N''-arylbenzamidrazones prepared from N-(phenylsulfonyl)benzohydrazonoyl chlorides and anilines.From the synthetic viewpoint for benzotriazines, this method may be of high utility on account of the availability of starting materials and higher yields.
- Ito, Suketaka,Tanaka, Yumo,Kakehi, Akikazu
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p. 859 - 864
(2007/10/02)
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