- Synthetic method N - (4 - fluoroaniline) -2 - hydroxyl - N - isopropyl acetamide
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The invention belongs to the technical field of medical intermediates, and particularly relates to a synthesis method N - (4 - fluoroaniline) -2 - hydroxyl - N - isopropylacetamide. To the invention, fluoronitrobenzene is used as a starting material, and hydrogenation is carried out. Condensation gives compound A, compound A is coupled to compound B by amide coupling, compound B is subjected to nucleophilic substitution reaction to give compound C, compound C is exchanged through ester exchange to obtain N - (4 - fluoroaniline) -2 - hydroxyl - N - isopropyl acetamide. The synthesis route of the complete N - (4 - fluoroaniline) -2 - hydroxyl - N - isopropyl acetamide is provided, and the synthesized N - (4 - fluoroaniline) -2 - hydroxyl - N - isopropyl acetamide is high in yield and high in purity.
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Paragraph 0015; 0017; 0021
(2021/10/02)
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- Preparation method of chemical intermediate N-isopropyl p-fluoroaniline
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The invention discloses a preparation method of a chemical intermediate that is N-isopropyl p-fluoroaniline, which is characterized in that the method comprises adding p-fluoronitrobenzene, a hydrogenation catalyst and acetone into a reaction kettle, heating to 55-75 DEG C, and introducing hydrogen into the reaction kettle to perform hydrogenation reduction reaction; after the reaction is finished, filtering the reaction system to recover the waste catalyst, and layering the filtrate obtained by filtering to obtain wastewater; and then performing rectification to obtain the target product N-isopropyl p-fluoroaniline; the hydrogenation catalyst is a composite catalyst, and the composite catalyst takes a nickel-doped carbon aerogel/TiO2 composite material as a carrier and Pt as a catalytic active component. The method disclosed by the invention is simple in process, economical, environment-friendly and high in product yield.
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Paragraph 0026-0067
(2020/05/08)
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- Flufenacet preparation method
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The invention discloses a flufenacet preparation method, which comprises synthesis of 2-methylsulfonyl-5-trifluoromethyl-1,3,4-thiadiazole, synthesis of 2-hydroxy-N-(4-fluoroaniline)-N-(1-methylethyl)acetamide and synthesis of 4'-fluoro-N-isopropyl-2-[5-(trifluridine)-1,3,4-thiadiazole-2-imide]acetamide. The optimal flufenacet preparation method is screened by a large number of experiments, the whole process is reasonable in design, particularly the steps of screening optimal reaction conditions and the optimal amount ratio, reaction temperature, reaction time and the like of reaction raw materials, the reaction yield (capable of reaching 90 percent or more) can be greatly increased, side reaction can be reduced, the reaction rate can be increased, the reaction raw materials can be recycled, the production cost is greatly reduced, and a broad application prospect is achieved.
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Paragraph 0036-0038
(2018/04/03)
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- Nickel(II) complex covalently anchored on core shell structured SiO2@Fe3O4 nanoparticles: A robust and magnetically retrievable catalyst for direct one-pot reductive amination of ketones
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A robust and efficient core shell structured magnetically retrievable nickel nanocatalytic system was fabricated via the covalent immobilization of 2-acetyl furan on the surface of an amine functionalized silica coated magnetic nanosupport followed by its metallation with nickel acetate. The newly synthesized magnetic silica based organic-inorganic hybrid nanocatalyst (Ni-ACF@Am-SiO2@Fe3O4) was systematically affirmed using several physico-chemical characterization tools such as FT-IR, XRD, VSM, SEM, TEM, EDS, ED-XRF and AAS. Thereafter, the catalytic performance of this Ni-ACF@Am-SiO2@Fe3O4 nanocatalyst was investigated in the one-pot reductive amination of ketones using NaBH4 as the reductant under neat conditions. The developed core shell magnetic silica based nickel nanocatalyst successfully afforded a structurally diverse range of secondary amines with high turnover frequency (TOF) and excellent conversion percentage. Additionally, it was found that this catalyst could not only be retrieved from the reaction vessel within a fraction of seconds using an external magnet but also be recycled for multiple runs without any discernible loss in its activity that rendered this protocol superior to all the previously established methodologies for the one-pot synthesis of substituted amines. Besides, some of the other fascinating features of this methodology that made it a potential candidate for addressing various economic and environmental concerns were ambient reaction conditions, broad substrate scope, simple workup procedure, shorter reaction time and cost effectiveness.
- Sharma, Rakesh Kumar,Dutta, Sriparna,Sharma, Shivani
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p. 2089 - 2101
(2016/03/19)
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- A N-isopropyl-4-fluoro aniline method for the preparation of
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The invention discloses an N-isopropyl-4-fluoroaniline preparation method. The preparation method comprises the following steps: adding 1 valent weight of 4-fluoronitrobenzene and 1-5 times of a mole valent weights of a compound (I), adding a transition metal catalyst having a total mass percentage of 0.2-5% and sulfonic acid or carboxylic acid having a total mass percentage of 0.1-10%, and reacting in the presence of an organic solvent in hydrogen environment at 30-130DEG C to obtain N-isopropyl-4-fluoroaniline. The preparation method has the advantages of simple process, high yield and few three wastes, and is benefit for the industrial production.
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Paragraph 0016; 0020; 0021
(2016/10/07)
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- Synthesis and herbicidal activity of N-aryl-2-heteroaryloxy-N-isopropyl acetamide
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A series of novel N-aryl-2-heteroaryloxy-N-isoproylacetamide derivatives were synthesized by multi-step reactions. Their structures were characterized by 1H NMR, MS and elemental analyses. The target compounds were evaluated for their herbicidal activities against Echinochloa crusgalli, Digitaria sanguinalis Scop., Abutilon theophrasti, Setaria viridis, Zinnia elegans and Acalypha australis. The results indicated that some of the title compounds displayed excellent herbicidal activities.
- Ye, Qing,Zhu, Xiao-Bo,Gu, Kai,Ni, Xiao-Quan,Gao, Jian-Rong,Wei-Rong, Miao
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p. 6931 - 6934
(2013/07/26)
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- Direct amination of phenols under metal-free conditions
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Herein, we disclose the metal-free synthesis of arylamines via the direct amination of phenols using aminating reagents. This reaction procedure uses easy accessible aminating reagents and provides a versatile synthetic route to a broad range of arylamines with various functionalities in good to excellent yield. By using a two-step route of amination and oxidative coupling reaction, we synthesized three naturally occurring carbazole alkaloids: murrayafoline A, mukonine, and clausenine from two commercially available phenols. Georg Thieme Verlag Stuttgart · New York.
- Yu, Jianzhong,Wang, Yongtao,Zhang, Peizhi,Wu, Jun
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supporting information
p. 1448 - 1454
(2013/07/26)
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- Cobalt-catalyzed electrophilic amination of arylzincs with N-chloroamines
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Roles reversed: An efficient cobalt-catalyzed electrophilic amination of arylzinc reagents has been achieved. A variety of functionalized arylzincs and N-chloroamines were coupled under mild conditions (see scheme). Both secondary and tertiary arylamines were obtained in moderate to excellent yields. Copyright
- Qian, Xin,Yu, Zailu,Auffrant, Audrey,Gosmini, Corinne
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supporting information
p. 6225 - 6229
(2013/07/05)
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- Zinc-promoted, iridium catalyzed reductive alkylation of primary amines with aliphatic ketones in aqueous medium
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The reductive alkylation of primary aromatic and aliphatic amines with aliphatic ketones has been achieved in aqueous acidic medium using commercially available, non-activated zinc dust catalyzed by a very small quantity of iridium bromide. Anilines react well in aqueous formic acid, whereas monoalkylamines require 1,4-dioxane as a co-solvent and sulfuric acid as the proton source. A plausible mechanism via low-valent iridium hydride species is proposed.
- da Silva, Renato A.,Bieber, Lothar W.
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scheme or table
p. 689 - 691
(2010/04/02)
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- S1P RECEPTORS MODULATORS AND THEIR USE THEREOF
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The invention relates to novel compounds that have S1P receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as autoimmune response.
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Page/Page column 74
(2010/04/30)
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- Hydroxycarboxylic acid anilides
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The present invention relates to a process for the preparation of hydroxycarboxylic acid amides of the general formula (1): STR1 in which R1 and R2 are identical or different and are hydrogen, halogen, cyano, a linear or branched alkyl, alkenyl, alkynyl or alkoxy group having 1 to 12 carbon atoms, an aralkyl group having 7 to 12 carbon atoms, a cycloalkyl group having 6 to 12 carbon atoms or an aryl group having 6 to 12 carbon atoms, R3 is hydrogen or a linear or branched alkyl group having 1 to 4 carbon atoms, R4 is hydrogen or a linear or branched alkyl group having 1 to 6 carbon atoms, or R3 and R4, together with the carbon atom to which they are attached, form a five- or six-membered cycloalkane ring, and n is an integer from 1 to 12, wherein an aniline of the general formula (2) STR2 in which R1, R2, R3 and R4 are as defined in the formula (1), is reacted with a hydroxycarboxylic acid of the general formula (3) STR3 in which n is as defined in the formula (1), in the presence or absence of an inert solvent, at 150° to 250° C., and the constituents which are volatile under the reaction conditions are distilled out of the reaction mixture.
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- Process for the preparation of glycoloylanilides
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A process for the preparation of glycoloylanilide of the formula (G) STR1 is recited that involves reacting a nitrobenzene with hydrogen and, if desired, with a carbonyl compound, in the presence of a noble metal catalyst and a solvent, reacting the compound produced with chloroacetyl chloride, reacting the resulting product with a benzyl alcohol and with a base, or reacting the resulting compound with an O-benzylglycoloyl chloride, and debenzylating the resulting benzylglycoloylanilide product by reacting with hydrogen in the presence of a noble metal catalyst. The invention also relates to a process for the preparation of O-benzylglycoloylanilide.
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- N-Isopropylcarbanilylmethyl dithiophosphates
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A class of compounds having the structural formula STR1 in which Ar is substituted phenyl and R is methyl or ethyl possesses improved activity as pre-emergent herbicides and insecticides.
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