- Characterization of degradation products of regorafenib by LC-QTOF-MS and NMR spectroscopy: Investigation of rearrangement and odd-electron ion formation during collision-induced dissociations under ESI-MS/MS
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Regorafenib is an oral multikinase inhibitor, and it was subjected to stress conditions (hydrolysis, oxidative, thermal and photolytic) as per ICH specified conditions. The drug showed considerable degradation under hydrolysis (acidic, basic and neutral) and oxidative stress conditions, whereas it was stable under other stress conditions. A total of five degradation products (DPs) were observed and these were analyzed by using a UHPLC-DAD system. Chromatographic separation was achieved on an Acquity CSH C18 column (100 × 2.1 mm, 1.7 μ) using 0.1% formic acid and acetonitrile:methanol (80:20%, v/v) as the mobile phase in gradient mode. All DPs were characterized by LC-MS/MS, and the major degradation product (DP1) was isolated by using an HPLC preparative system from a degradation mixture and analyzed using NMR (1D and 2D NMR) and IR experiments. It was observed that protonated DP1 and DP3 undergo rearrangement reactions during collision-induced dissociations under positive electrospray ionization conditions. Additionally, in silico toxicity of the drug and its degradation products (DP1-DP5) was evaluated using TOPKAT and DEREK toxicity prediction software tools.
- Baira, Shandilya Mahamuni,Srinivasulu, Gannoju,Nimbalkar, Rakesh,Garg, Prabha,Srinivas,Talluri, M.V.N. Kumar
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Read Online
- Preparation and characterization of diazenyl quinolin-8-ol with trifluoromethyl substituents
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The synthesis and properties of new monoazo dyes derived from the diazonium salts of 2-trifluoromethyl phenylamine and 4-chloro-3-trifluoromethyl phenylamine are considered.
- Yazdanbakhsh, Mohammad R.,Mahmoodi, Nosrat O.,Dabiry, Shahram
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Read Online
- Catalytic production of anilines by nitro-compounds hydrogenation over highly recyclable platinum nanoparticles supported on halloysite nanotubes
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Pt-nanoparticles supported on halloysite-nanotubes (HNTs) were selectively deposited onto the inner (Pt(IN)/HNT) or outer (Pt(OUT)/HNT) surface of the support to evaluate their operational stability on the cleaner and efficient hydrogenation of nitro compounds to produce their corresponding anilines. The formation of Pt0-aggregates on the inner or outer surfaces was observed, with mean particles sizes of 2.4–2.9 nm. The catalysts were evaluated using ethanol as solvent and nitrobenzene as a model substrate at a temperature of 298 K, under 1 bar of H2 pressure. The Pt(IN)/HNT catalyst showed better catalytic performance than Pt(OUT)/HNT, which was mainly attributed to the confinement effect of the Pt-nanoparticles inside the HNTs. However, the operational stability showed that Pt(OUT)/HNT retained its catalytic performance after 15 cycles, while the Pt(IN)/HNT catalyst suffered deactivation after the 5th cycle. The best catalytic system showed a moderate-to-high efficiency in the efficient hydrogenation of 7 nitro compounds used to produce their corresponding anilines, which are important pharmaceutical building blocks.
- Aepuru, Radhamanohar,Bustamante, Tatiana M.,Campos, Cristian H.,Leal-Villarroel, Edgardo,Mangalaraja, Ramalinga Viswanathan,Shanmugaraj, Krishnamoorthy,Torres, Cecilia C.,Vinoth, Victor
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- Noble metal nanoparticles supported on titanate nanotubes as catalysts for selective hydrogenation of nitroarenes
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Platinum (Pt) and palladium (Pd) nanoparticles (NPs) supported on titanate nanotubes (TiNTs) Pt@TiNT and Pd@TiNT were prepared for the liquid-phase hydrogenation of nitroarenes at 25 °C Initially, TiNT was modified with 3-aminopropyl-trimethoxysilane to provide a strong anchoring site to trap the Pt and Pd NPs, which prevent the metal NPs from leaching. As-prepared 1 wt% of metal loading catalysts were characterized by transmission electron microscopy (TEM), nitrogen adsorption–desorption isotherms, X-ray diffraction, and X-ray photoelectron spectroscopy measurements. The TEM images confirmed that the Pt (1.70 ± 0.19 nm) and Pd (2.80 ± 0.43 nm) NPs were mainly confined into the channel of TiNTs. Both catalysts exhibited excellent catalytic performances for the reduction of nitrobenzene as a model compound under mild reaction conditions. The superior catalytic activity for the hydrogenation of nitroarenes is attributed to the small size of the Pt and Pd NPs. However, the operational stability showed that Pt@TiNT retained its catalytic performance after 10 cycles, while Pd@TiNT suffered deactivation by metal sintering after the sixth cycle. The Pt@TiNT system exhibited high efficiency in the hydrogenation of different substituted nitroarenes of pharmaceuticals interest, and it showed an excellent activity and selectivity toward the production of desired substituted anilines.
- Aepuru, Radhamanohar,Bustamante, Tatiana M.,Campos, Cristian H.,Mangalaraja, Ramalinga Viswanathan,Shanmugaraj, Krishnamoorthy,Torres, Cecilia C.,de León, J. N. Díaz
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- Commercially Available CuO Catalyzed Hydrogenation of Nitroarenes Using Ammonia Borane as a Hydrogen Source
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Tandem ammonia borane dehydrogenation and nitroarenes hydrogenation has been reported as a novel strategy for the preparation of aromatic amines. However, the practical application of this strategy is subjected to the high-cost and tedious preparation of supported noble metal nanocatalysts. The commercially available CuO powder is herein demonstrated to be a robust catalyst for hydrogenation of nitroarenes using ammonia borane as a hydrogen source under mild conditions. Numerous amines (even sterically hindered, halogenated, and diamines) could be obtained through this method. This monometallic catalyst is characteristic of support-free, excellent chemoselectivity, low-cost, and high recyclability, which will favor its future utilization in preparative reduction chemistry. Mechanistic studies are also carried out to clarify that diazene and azoxybenzene are key intermediates of this heterogeneous reduction.
- Du, Jialei,Chen, Jie,Xia, Hehuan,Zhao, Yiwei,Wang, Fang,Liu, Hong,Zhou, Weijia,Wang, Bin
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p. 2426 - 2430
(2020/03/30)
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- Cobalt oxide NPs immobilized on environmentally benign biological macromolecule-derived N-doped mesoporous carbon as an efficient catalyst for hydrogenation of nitroarenes
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Highly nitrogen-doped mesoporous carbon (N-mC) material incorporated cobalt oxide nanoparticles was synthesized through simple pyrolysis of environmentally friendly chitosan-polyaniline-Co(OAc)2 precursor in one-step. The as-prepared catalyst named CoO&at;N-mC with 14.65 ?wtpercent nitrogen content was characterized by different analysis techniques. The heterogeneous catalyst exhibits outstanding catalytic activity for the reduction of a variety of nitroaromatic compounds in the presence of NaBH4 as a reducing agent in water as a green solvent at 75 ?°C. Utilization of natural biological macromolecules such as chitosan as green and cheap starting material with harmless aniline and earth-abundant cobalt salt, facile synthesis, excellent product yield, short reaction time, high chemoselectivity, sustainable and mild reaction condition, and reusability of catalyst for at least five cycles without any significant decline in the catalytic efficiency are some prominent merits of this new nanocatalyst.
- Elhampour, Ali,Nanadegani, Zahra Soleimani,Nemati, Firouzeh,Rangraz, Yalda
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- Regorafenib analogues and their ferrocenic counterparts: Synthesis and biological evaluation
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Approved by the FDA in 2012, regorafenib is one of the last chance treatments for colorectal cancer. While various analogues have already been prepared, ferrocenic derivatives have never been evaluated. In this study, we prepared various ferrocene-containing derivatives of regorafenib and recorded their biological activity in kinase and cellular assays. This led to the identification of a squaramide derivative which shows a good cellular activity and three ferrocene analogues with promising activity in both kinase and cellular assays. This journal is
- Wilde, Myron,Arzur, Danielle,Baratte, Blandine,Lefebvre, Dorian,Robert, Thomas,Roisnel, Thierry,Le Jossic-Corcos, Catherine,Bach, Stéphane,Corcos, Laurent,Erb, William
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supporting information
p. 19723 - 19733
(2020/12/04)
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- Pd-Co catalysts prepared from palladium-doped cobalt titanate precursors for chemoselective hydrogenation of halonitroarenes
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Bimetallic Pd-Co catalysts supported on the mixed oxides CoTiO3-CoO-TiO2 (CTO) were synthesized via the thermal reduction of Pd-doped cobalt titanates PdxCo1-xTiO3 and evaluated for the chemoselective hydrogenation of halonitroarenes to haloarene-amines. The nominal Pd mass percentage of the Pd-Co/CTO systems was varied from 0.0 to 0.50. After the thermal reduction of PdxCo1-xTiO3 at 500 °C for 3 h, Pd was completely reduced and Co was partially reduced, producing a mixture of ionic Co, metallic Co, and TiO2-rutile species to give the supported bimetallic catalysts. The metallic cobalt content increased with the Pd content of the precursor. The catalytic activity toward 4-chloronitrobenzene increased with the Pd content; however, >0.1 mass% Pd decreased the chemoselectivity toward 4-chloroaniline due to the formation of the hydrodehalogenation product—aniline. The 0.1Pd-Co/CTO system was used as a model catalyst to produce haloarene-amine building blocks for linezolid, loxapine, lapatinib, and sorafenib with >98% conversion, 96% chemoselectivity, and no hydrohalogenation products. Finally, recycling tests of the 0.1Pd-Co/CTO catalyst showed loss of activity and selectivity during the third cycle due to catalyst deactivation. Regeneration treatments, every two catalytic cycles, allowed six operation cycles without loss of chemoselectivity and only a slight decrease in catalytic activity during the last cycle.
- Bustamante, Tatiana M.,Dinamarca, Robinson,Torres, Cecilia C.,Pecchi, Gina,Campos, Cristian H.
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- Synthesis method 4- chloro -3-(trifluoromethyl)-phenylisocyanate
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The invention belongs to the technical field of medicines, and concretely relates to 4 - chloro - 3 3 3 (trifluoromethyl) phenylisocyanate) synthesis method. o chlorotrifluorotoluene, acetic anhydride and concentrated nitric acid to obtain 4 - nitro - 2 2-trifluoromethyl chlorobenzene, 4 - nitro - 2 2-trifluoromethyl chlorobenzene, activated carbon, FeCl. 3 · 66H2 O And hydrazine hydrate react to obtain 4 - chlorine - 3 3-trifluoromethylaniline, 4 - chloride - 3 3-trifluoromethylaniline, triphosgene and a catalyst react to obtain 4 - chlorine - 3 3 3-trifluoromethyl)-phenylisocyanate . instead of the conventional nitric/sulfuric acid mixed acid system / reaction, risks low, nitrosation FeCl impurities, reduction process. 3 · 66H2 O/Activated carbon/hydrazine hydrate system replaces traditional iron powder reduction process, has avoided the production, of a large amount of iron mud waste residue and has reduced environmental protection pressure.
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Page/Page column 5; 6
(2020/03/29)
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- Promotional effect of palladium in Co-SiO2 core@shell nanocatalysts for selective liquid phase hydrogenation of chloronitroarenes
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This study describes the synthesis of palladium-promoted Co@SiO2 catalyst developed by electrostatic immobilization of Pd ionic precursor onto Co3O4 nanoparticles core, coated with a mesoporous SiO2 shell. The oxidized Pd-Co3O4@SiO2 (xPdCo-ox) and partially reduced Pd-Co@SiO2 (xPdCo-red) nanocatalysts were used in the direct synthesis of chloro-arylamines from chloronitroarenes employing heterogeneous hydrogenation process. The effect of palladium content (xPdCo; x = 0.0, 0.5, 1.0 and 3.0 Pd wt%) in the Co3O4 core of the structures on catalytic performance for the hydrogenation of 4-chloronitrobenzene (CNB) to 4-chloroaniline (CAN) was systematically studied. It was found that the incorporation of palladium ionic precursor promotes both Co3O4 core nanoparticles flocculation and an increase in the mesoporous shell thickness in the Pd-promoted catalysts compared to the pristine Co-SiO2 core-shell structure. The TPR, XRD, XPS and magnetic measurements results indicated that the palladium addition promoted the reduction of Co3O4 core during the isothermal H2 treatment at 873 K rendering metallic Pd° and Co° species. The catalytic CNB hydrogenation experiments showed that the 0.5PdCo-red catalyst inhibited both the hydrodechlorination and intermediates accumulation reaching 99% yield in CAN compared to 1.0PdCo-red and 3.0PdCo-red catalysts which provided aniline as undesired product. Additionally, the 0.5PdCo-red catalyst was easily recycled with a moderate catalytic activity after five consecutive reaction cycles. Finally, the catalytic hydrogenation performance of the 0.5PdCo-red catalyst for different pharmaceutical substituted chloro-nitroarenes such as 1-(4-chlorophenoxy)-2-nitrobenzene, 2-chloro-1-((3-fluorobenzyl)oxy)-4-nitrobenzene and 2-chloro-5nitrobenzotrifluoride was also evaluated and revealed high activity (>99% at 3 h of reaction) and selectivity towards the desired chloro-arylmines production, highlighting the potential of this catalyst in these processes.
- Bustamante, Tatiana M.,Campos, Cristian H.,Fraga, Marco A.,Fierro,Pecchi, Gina
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p. 224 - 237
(2020/04/08)
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- Oxalic amide ligands, and uses thereof in copper-catalyzed coupling reaction of aryl halides
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The present invention provides oxalic amide ligands and uses thereof in copper-catalyzed coupling reaction of aryl halides. Specifically, the present invention provides a use of a compound represented by formula I, wherein definitions of each group are described in the specification. The compound represented by formula I can be used as a ligand in copper-catalyzed coupling reaction of aryl halides for the formation of C—N, C—O and C—S bonds.
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Page/Page column 89-90
(2020/01/09)
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- HETEROCYCLIC CARBOXYLIC ACID AMIDE LIGAND AND APPLICATIONS THEREOF IN COPPER CATALYZED COUPLING REACTION OF ARYL HALOGENO SUBSTITUTE
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Provided are a heterocyclic carboxylic acid amide ligand and applications thereof in a copper catalyzed coupling reaction. Specifically, provided are uses of a compound represented by formula (I), definitions of radical groups being described in the specifications. The compound represented by formula (I) can be used as the ligand in the copper catalyzed coupling reaction of the aryl halogeno substitute, and is used or catalyzing the coupling reaction for forming the aryl halogeno substitute having C—N, C—O, C—S and other bonds.
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Paragraph 0266-0267
(2019/05/15)
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- The preparation method of the zola non-nepal (by machine translation)
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The invention discloses a method for preparing zola non-nepal, the states the zola non-nepal the chemical name is 4 - {4 - [( {4 - chloro - 3 - (trifluoromethyl) phenyl] amino} carbonyl) amino] phenoxy} - N - methylpyridine - 2 - carboxamide; the process of the invention has simple process, raw materials are easy, economic and environmental protection, help to realize industrialization, can promote the zola non-nepal drug of economic and technological development, and reduces the production cost, high yield, low environmental pollution, is suitable for mass production. (by machine translation)
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Paragraph 0012-0014
(2018/04/28)
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- AMINATION AND HYDROXYLATION OF ARYLMETAL COMPOUNDS
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In one aspect, the present disclosure provides methods of preparing a primary or secondary amine and hydroxylated aromatic compounds. In some embodiments, the aromatic compound may be unsubstituted, substituted, or contain one or more heteroatoms within the rings of the aromatic compound. The methods described herein may be carried out without the need for transition metal catalysts or harsh reaction conditions.
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Paragraph 0098; 0134; 0135; 0185
(2018/03/25)
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- Synergistic effects in Fe nanoparticles doped with ppm levels of (Pd + Ni). A new catalyst for sustainable nitro group reductions
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A remarkable synergistic effect has been uncovered between ppm levels of Pd and Ni embedded within iron nanoparticles that leads to mild and selective catalytic reductions of nitro-containing aromatics and heteroaromatics in water at room temperature. NaBH4 serves as the source of inexpensive hydride. Broad substrate scope is documented, along with several other features including: low catalyst loading, low residual metal in the products, and recycling of the catalyst and reaction medium, highlight the green nature of this new technology.
- Pang, Haobo,Gallou, Fabrice,Sohn, Hyuntae,Camacho-Bunquin, Jeffrey,Delferro, Massimiliano,Lipshutz, Bruce H.
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supporting information
p. 130 - 135
(2018/01/12)
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- Method for synthesizing 4-chloro-3-trifluoromethylaniline by micro-channel reactor
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The invention provides a method for synthesizing 4-chloro-3-trifluoromethylaniline by a micro-channel reactor, and belongs to the field of synthesis of anti-tumor type medicines in organic synthesis.The invention solves the problems of low yield, poor purity, high energy consumption, danger caused by easy occurrence of severe explosion, degradation caused by long reaction time at high temperatureand high pressure, low catalyst recycling frequency and the like existing in the traditional synthesis method, and provides a method for synthesizing 4-chloro-3-trifluoromethylaniline by a micro-channel reactor. The method particularly comprises the following steps: 1) enabling O-chlorbenzotrifluoride to be subjected to nitration reaction with the mixture of concentrated sulfuric acid and concentrated nitric acid in a reaction module of the micro-channel reactor, and performing after-treatment to obtain 2-chloro-5-nitrobenzotrifluoride; and 2) adding the 2-chloro-5-nitrobenzotrifluoride to anorganic solvent to be dissolved, then adding an active carbon noble metal catalyst and phosphorous acid, adding the components to a preheating module to be mixed and preheated, enabling the preheatedmixture to be subjected to reaction with H2 in the reaction module, and performing after-treatment to obtain 4-chloro-3-trifluoromethylaniline. The method provided by the invention is suitable for large-scale production of 4-chloro-3-trifluoromethylaniline.
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Paragraph 0047; 0050; 0053; 0056; 0057-0059; 0062-0068
(2018/07/30)
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- Synthesis of sulfamide analogues of deoxthymidine monophosphate as potential inhibitors of mycobacterial cell wall biosynthesis
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The recently discovered enzyme Mycobacterium tuberculosis thymidine monophosphate kinase (TMPKmt), which catalyses the phosphorylation of deoxythymidine monophosphate (dTMP) to give deoxythymidine diphosphate (dTDP), is indispensable for the growth and survival of M. tuberculosis as it plays an essential role in DNA synthesis. Inhibition of TMPKmt is an attractive avenue for the development of novel anti-tuberculosis agents. Based on the premise that sulfamide may be a suitable isostere of phosphate, deoxythymidine analogues comprising various substituted sulfamides at C5′ were modelled in silico into the active site of TMPKmt (PDB accession code: 1N5K) using induced-fit docking methods. A selection of modelled compounds was synthesized, and their activity as inhibitors of TMPKmt was evaluated. Three compounds showed competitive inhibition of TMPKmt in the micromolar range (10–50 μM). Compounds were tested in vitro for anti-mycobacterial activity against M. smegmatis: three compounds showed weak anti-mycobacterial activity (MIC 250 μg/mL).
- Suthagar, Kajitha,Jiao, Wanting,Munier-Lehmann, Hélène,Fairbanks, Antony J.
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- FE NANOPARTICLES WITH PPM CONTENTS OF PD, CU AND/OR NI, REACTIONS IN WATER CATALYZED BY THEM
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The present application discloses a nanoparticle composition prepared from a mixture comprising: a) a transition metal salt; b) an iron salt; and c) a reducing agent; and methods for the use of such compositions, including the reduction of an organic compound comprising a nitro group to form an organic compound comprising an amine group, the Cu-catalyzed cyclization of an azide and an alkyne (click chemistry) and cross coupling reactions, notably Suzuki-Miyaura reactions. The transition metal salts are in particular Pd, Cu and Ni salts, the content of these metals being typically in the ppm range based on the major constituent Fe in the final products.
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Paragraph 0084; 0088
(2017/07/14)
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- Rapid heteroatom transfer to arylmetals utilizing multifunctional reagent scaffolds
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Arylmetals are highly valuable carbon nucleophiles that are readily and inexpensively prepared from aryl halides or arenes and widely used on both laboratory and industrial scales to react directly with a wide range of electrophiles. Although C-C bond formation has been a staple of organic synthesis, the direct transfer of primary amino (-NH2) and hydroxyl (-OH) groups to arylmetals in a scalable and environmentally friendly fashion remains a formidable synthetic challenge because of the absence of suitable heteroatom-transfer reagents. Here, we demonstrate the use of bench-stable N-H and N-alkyl oxaziridines derived from readily available terpenoid scaffolds as efficient multifunctional reagents for the direct primary amination and hydroxylation of structurally diverse aryl- and heteroarylmetals. This practical and scalable method provides one-step synthetic access to primary anilines and phenols at low temperature and avoids the use of transition-metal catalysts, ligands and additives, nitrogen-protecting groups, excess reagents and harsh workup conditions.
- Gao, Hongyin,Zhou, Zhe,Kwon, Doo-Hyun,Coombs, James,Jones, Steven,Behnke, Nicole Erin,Ess, Daniel H.,Kürti, László
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p. 681 - 688
(2017/06/30)
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- Safe and Selective Nitro Group Reductions Catalyzed by Sustainable and Recyclable Fe/ppm Pd Nanoparticles in Water at Room Temperature
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As a result of a unique synergy between ligand-free Fe/ppm Pd nanoparticles and PEG-containing designer surfactants, a facile and selective reduction of nitro-containing aromatics and heteroaromatics can be effected in water at room temperature in the presence of NaBH4. This new nanotechnology involves low catalyst loadings, is highly chemoselective, and tolerates a wide variety of functional groups. The process, which includes recycling of the entire aqueous medium, offers a general, environmentally responsible, and notably safe approach to highly valued reductions of nitro-containing compounds.
- Feng, Jie,Handa, Sachin,Gallou, Fabrice,Lipshutz, Bruce H.
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supporting information
p. 8979 - 8983
(2016/07/26)
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- Assembly of Primary (Hetero)Arylamines via CuI/Oxalic Diamide-Catalyzed Coupling of Aryl Chlorides and Ammonia
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A general and practical catalytic system for aryl amination of aryl chlorides with aqueous or gaseous ammonia has been developed, with CuI as the catalyst and bisaryl oxalic diamides as the ligands. The reaction proceeds at 105-120°C to provide a diverse set of primary (hetero)aryl amines in high yields with various functional groups.
- Fan, Mengyang,Zhou, Wei,Jiang, Yongwen,Ma, Dawei
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supporting information
p. 5934 - 5937
(2015/12/11)
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- Mild and highly selective palladium-catalyzed monoarylation of ammonia enabled by the use of bulky biarylphosphine ligands and palladacycle precatalysts
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A method for the Pd-catalyzed arylation of ammonia with a wide range of aryl and heteroaryl halides, including challenging five-membered heterocyclic substrates, is described. Excellent selectivity for monoarylation of ammonia to primary arylamines was achieved under mild conditions or at rt by the use of bulky biarylphosphine ligands (L6, L7, and L4) as well as their corresponding aminobiphenyl palladacycle precatalysts (3a, 3b, and 3c). As this process requires neither the use of a glovebox nor high pressures of ammonia, it should be widely applicable.
- Cheung, Chi Wai,Surry, David S.,Buchwald, Stephen L.
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supporting information
p. 3734 - 3737
(2013/08/23)
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- Regioselective chlorination and bromination of unprotected anilines under mild conditions using copper halides in ionic liquids
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By using ionic liquids as solvents, the chlorination or bromination of unprotected anilines at the para-position can be achieved in high yields with copper halides under mild conditions, without the need for potentially hazardous operations such as supplementing oxygen or gaseous HCl.
- Wang, Han,Wen, Kun,Nurahmat, Nurbiya,Shao, Yan,Zhang, He,Wei, Chao,Li, Ya,Shen, Yongjia,Sun, Zhihua
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supporting information; experimental part
p. 744 - 748
(2012/06/30)
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- Synthesis, characterization and derivatization of some novel types of mono- and bis-imidazolidineiminothiones and imidazolidineiminodithiones with antitumor, antiviral, antibacterial and antifungal activities - part I
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Halogenated and alkylated N-arylcyanothioformanilides were reacted with the nucleophilic reagents triethylamine, hydrazine and diphenyldiazomethane to produce N-arylcyanothioformanilide ammonium salts, a thiosemicarbazide and a 2-(arylamino)-3,3-diphenylacrylonitrile, respectively. They also underwent several types of electrophilic reactions with aryl-, arylbisisocyanates and arylisothiocyanates to yield mono- and bis-imidazolidineiminothiones and imidazolidineiminodithiones. Treatment of imidazolidineiminothiones with hydrogen sulfide, substituted ortho-phenylenediamines and thiocarbohydrazide afforded the corresponding thiohydantoin, quinoxaline and imidazotriazine derivatives. Several of the synthesized products were subjected to in vitro biological evaluation against antitumor, antiviral, antimicrobial and antifungal strains. Most tested compounds showed significant activities.
- El-Sharief, Ahmed M. Sh.,Moussa, Ziad
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experimental part
p. 4315 - 4334
(2009/12/24)
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- Aryl ureas with angiogenisis inhibiting activity
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This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.
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- Aryl ureas as kinase inhibitors
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This invention relates to new aryl ureas and methods for their synthesis. The inventive compounds are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.
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- Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
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This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.
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- TRACE ENRICHMENT TECHNIQUE USING AMBERLITE XAD-2 RESIN AND APPLICATION TO TRICLOCARBAN, CLOFLUCARBAN AND RELATED COMPOUNDS
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Amberlite XAD-2 has been used to preconcentrate trace amounts of carbanilides in pure water.A high percent recovery was found for these compounds, but recovery depended on the symmetry around the carbonyl group.Application of this resin to concentrate the degraded components showed that under acidic and basic conditions these carbanilides primarily degraded into substituted anilines.It was found that photohydrolysis of the carbanilides studied produced the expected substituted anilines, except for cloflucarban, which gave p-chloro-m-aminobenzoic acid instead of theexpected p-chloro-m-trifluoromethylaniline.All separations and analyses of the carbanilides and products were done using linear temperature programmed GLC after derivatization with N-methyl-N-(trimethylsilyl)-trifluoroacetamide (MSTFA).
- Audu, Aramani A.
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p. 603 - 608
(2007/10/02)
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