- Design, solvent-free synthesis and antibacterial activity evaluation of new coumarin sulfonamides
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A simple cost-effective and green method was presented for the synthesis of coumarin bis sulfonamides. Seventeen novel coumarin sulfonamides were synthesized in good to high yield and purity in six steps starting from 2-amino thiazole, aniline, and 4-methoxy aniline. All of the reactions have been done under green conditions without using any hazardous solvent. The chemical structures of the products were elucidated by IR, 1H NMR, and 13C NMR spectroscopy and elemental analysis. Also, the anti-bacterial properties of the synthesized sulfonamides were investigated using two strains of Staphylococcus (gram-positive) and Escherichia coli (gram-negative) bacteria.
- Aminarshad, Farzaneh,Heidari, Shima,Mostajeran, Neda,Massah, Ahmad Reza
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p. 547 - 562
(2021/08/16)
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- Direct synthesis of N-arylamides via the coupling of aryl diazonium tetrafluoroborates and nitriles under transition-metal-free conditions
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The direct synthesis of N-arylamides via the coupling of aryl diazonium tetrafluoroborates and nitriles under transition-metal-free conditions has been developed. The reported protocol is practical and represents an efficient method to produce functionalized amides in moderate to good yields.
- Xiong, Biquan,Wang, Gang,Xiong, Tao,Wan, Liming,Zhou, Congshan,Liu, Yu,Zhang, Panliang,Yang, Changan,Tang, Kewen
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supporting information
p. 3139 - 3142
(2018/07/13)
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- Eco-friendly, catalyst and solvent-free, synthesis of acetanilides and N-benzothiazole-2-yl-acetamides
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An expeditious and green synthesis of acetamides in a solvent-free simple way is described, without catalyst or additives, and in good yield by an instantaneous reaction of anilines or 2-aminothiazoles and acetic anhydride without external heating, and with simple purification. Sixteen substituted acetanilides and four N-benzothiazole-2-yl-acetamides were formed, but aliphatic amines of low molecular weight were not as effective as aromatic ones, and only cyclohexylamine and the enaminone ethyl 3-amino-2-butenoate afforded the corresponding acetamides in good yield.
- Cunha, Silvio,De Santana, Louren?o L. B.
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p. 1137 - 1144
(2017/05/01)
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- NOVEL COMPOUNDS
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The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.
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Page/Page column 100
(2016/04/20)
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- Magnetically separable γ-Fe2O3 nanoparticles: An efficient catalyst for acylation of alcohols, phenols, and amines using sonication energy under solvent free condition
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This paper reports a facile synthesis of magnetically separable iron oxide (γ-Fe2O3) nanoparticles using thermolysis method. The structural and morphological study of the synthesized γ-Fe2O3 nanoparticles was carried out using X-ray diffraction (XRD), field emission gun-scanning electron microscopy (FEG-SEM), energy dispersive X-ray spectrum (EDS), transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), and X-ray photoelectron spectroscopy (XPS) techniques. The electron microscopy reveals that the γ-Fe2O3 nanoparticles have spherical morphology with a particle size in the range of 40-100 nm. The XPS study confirmed the Fe is in +3 oxidation state. The synthesized γ-Fe2O3 nanoparticles have been used as an efficient heterogeneous catalyst for the organic transformation between phenols, alcohols, and amines with acetic anhydride under sonication using mild reaction conditions. Various electrons withdrawing and electrons donating substrates show an excellent yield of desired products with the advantage of magnetic separation and reusability of γ-Fe2O3 nanocatalyst.
- Bhosale, Manohar A.,Ummineni, Divya,Sasaki, Takehiko,Nishio-Hamane, Daisuke,Bhanage, Bhalchandra M.
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- Chemoselective N-deacetylation under mild conditions
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A mild and efficient chemoselective N-deacetylation using the Schwartz reagent at room temperature in rapid time is described. The mild and neutral conditions enable orthogonal N-deacetylation in the presence of some of the common protecting groups (viz. Boc, Fmoc, Cbz, Ts). The deprotection conditions did not induce any epimerization at the chiral amino centre.
- Sultane, Prakash R.,Mete, Trimbak B.,Bhat, Ramakrishna G.
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supporting information
p. 261 - 264
(2014/01/06)
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- Microwave-assisted synthesis of amide under solvent-free conditions
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An efficient and environmentally friendly synthetic method for the synthesis of primary amides under microwave irradiation was described, in which the primary amine was directly reacted with acid without any catalytic agents. The reaction took place in 8-12-min, which was much shorter than the traditional synthetic methods, with almost quantitative yields. The influential factor of the reaction was discussed. The tautomerization between the carboxylic acid group and the H atom in α-carbon of L-amino acid was observed, presumably a dehydrated intermediate forming from this tautomerized isomer. Copyright Taylor & Francis Group, LLC.
- Wang, Xiao-Jian,Yang, Qian,Liu, Fei,You, Qi-Dong
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p. 1028 - 1035
(2008/09/18)
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- Synthetic Study Directed Toward Novel Multi-Linked Heterocycles
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2-Amino-4-(1-methylindol-3-yl)thiazole (11c) has a characteristic nucleophilic nature at the 5-position and add to the 4-position of acetylpyridinium acetate (13) producing 2-acetylamino-5-(1-acetyl-1,4-dihydropyridin-4-yl)-4-(1-methylindol-3-yl)-thiazole (1c).Its structure was established by X-ray single crystallographic analysis.Applying the results, simple syntheses of the related tris- (1a-b and 2-8) and tetrakislinked heterocycles (9) were achieved.
- Somei, Masanori,Yamada, Yoshikazu,Kitagawa, Keiichi,Sugaya, Katsuko,Tomita, Yayoi,et. al
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p. 434 - 438
(2007/10/03)
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- Amide anions as unexpected activating groups in nucleophilic heteroaromatic substitution
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Nucleophilic displacement of halide by alkoxide in pyridazines, phthalazines, a thiazole and a thiadiazole is unexpectedly activated by acetamido anion substituents compared to neutral amido and amino substituents.
- Gillies,Gillies, Iain,Rees,Rees, Charles W.
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p. 4065 - 4068
(2007/10/03)
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- SYNTHESIS OF N-ACETYL-N'-ARYL(HETERYL)UREAS FROM N-(1-HYDROXYIMINO-2-OXOPROPYL)PYRIDINIUM CHLORIDE
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N-Acetyl-N'-aryl(heteryl)ureas were synthesized by reaction of N-(1-hydroxyimino-2-oxopropyl)pyridinium chloride with amines.The use of amines on a silica support considerably increases the yield of acetylureas.
- Poplavskaya, I. A.,Aubakirova, G. B.,Kurmangalieva, R. G.
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p. 425 - 431
(2007/10/03)
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- Reaction of 2-Aminothiazoles with Reagents containing a C-Halogen and a C=O Electrophilic Centre
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Seven reagents of different types having in common a C-Hal and a C=O electrophilic centre have been used in a study of their reactions with 2-aminothiazoles.Three reagents, CHBrAc2 and ROCHBrCO2Et (R = Me, Ph), gave imidazothiazoles, thus providing useful routes to the 5-acetyl and 5-ethoxycarbonyl derivatives.Unexpectedly, the solvent (acetone) was involved in the reaction of the fourth reagent, CHBr(CO2Et)2, with 2-aminothiazole which led to 5,5-di(ethoxycarbonyl)-6,6-dimethyl-5,6-dihydroimidazothiazole (yield 81percent).With the last three reagents (AcCHBrNO2, BzCHBrCN and ICH2CO2C6H4NO2-p) the outcome was simpler, viz., the formation of 2-amidothiazoles.It is proposed that electrophilic attack by the endo-N of the 2-aminothiazole is the first step in all cases.This occurs at the C-Hal centre of the first four reagents and is followed by cyclisation to the exo-N.In the last three electrophiles the presence of the groups well suited to leaving as stabilised anions favours addition to the C=O group; the intermediates so formed subsequently isomerise to the more stable exo-N substituted products.
- Compton, Victoria J.,Meakins, G. Denis,Raybould, Amanda J.
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p. 2029 - 2032
(2007/10/02)
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