35613-44-6Relevant articles and documents
Synthesis process of diclofenac sodium
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, (2021/09/26)
The invention provides a synthesis process of diclofenac sodium, which is obtained by acylation reaction of o-aminobenzene acetate with 2 and 6 - dichlorophenoxy acetic acid respectively and acylation with chlorobenzoyl chloride followed by nucleophilic substitution with 2, 6 - dichlorophenol or 2 and 6 -dichlorophenol. Is hydrolyzed to give sodium diclofenac sodium. The synthesis process is simplified, the reaction condition is mild, and the yield and industrial popularization and application are facilitated.
NovelN-transfer reagent for converting α-amino acid derivatives to α-diazo compounds
Lu, Guan-Han,Huang, Tzu-Chia,Hsueh, Hsiao-Chin,Yang, Shin-Cherng,Cho, Ting-Wei,Chou, Ho-Hsuan
supporting information, p. 4839 - 4842 (2021/05/25)
A novel universalN-transfer reagent for direct and effective transformation of α-amino ketones, acetamides, and esters to the corresponding α-diazo products under mild basic conditions has been developed. This one-step synthetic approach not only allows for generation of α-substituted-α-diazo carbonyl compounds from α-amino acid derivatives but also permits preparation of α-diazo dipeptides fromN-terminal dipeptides (32 examples, up to 91%).
Gold(I)-Thiolate Oligomers for Catalytic Hydrogenation of Nitroaromatics in Aqueous and Organic Medium
You, Jyun-Guo,Jin, Dun-Yuan,Tseng, Wei-Bin,Tseng, Wei-Lung,Lin, Po-Chiao
, p. 4558 - 4567 (2020/08/19)
Thiolated gold nanoclusters (AuNCs) have been introduced to efficiently and selectively catalyze the hydrogenation of nitroaromatics due to the strong interaction of their S?Au-S staple motifs with the nitro groups of nitroaromatics. However, without a gold core, gold(I)-thiolate oligomers (AuSOs) with S?Au-S staple motifs are rarely explored as catalysts for nitroaromatics. Here, we report a straightforward strategy for the synthesis of AuSOs through hydroxyl radical-induced leaching of glutathione-capped gold nanoparticles (GSH-AuNPs). Raman spectroscopy and matrix-assisted laser desorption/ionization-time of flight mass spectrometry demonstrated that hydroxyl radical-triggered etching of the GSH-AuNPs resulted in the production of AuSOs, including Au4(GSH)7 and Au7(GSH)9. The AuSOs were found to catalyze NaBH4-mediated hydrogenation of 4-nitrophenol to 4-aminophenol with a chemoselectivity of ~100 percent and a normalized rate constant (Knor) of 4.8×105 s? g?1. In addition to the high affinity of the S?Au?S staple motifs for 4-nitrophenol, the unusual catalytic activity of the AuSOs was attributable to the fact that they efficiently catalyzed the production of H2 from NaBH4 and the reaction of dissolved oxygen and NaBH4. The chemoselectivity and applicability of the AuSOs were further verified by performing the catalytic reaction of methyl 2-(2-nitrophenyl) acetate or methyl 4-nitrobenzoate with NaBH4.
Synthetic method of poly-substituted dimethyl amino phenyl acetic acid compound
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Paragraph 0046-0049; 0088-0091, (2021/03/05)
The invention relates to a synthesis method of a poly-substituted dimethyl amino phenyl acetic acid compound. The synthesis method comprises the following steps: carrying out methyl esterification reaction on a compound shown in a formula I to obtain a co
A synthesis method of diclofenac (by machine translation)
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Paragraph 0052; 0058; 0059, (2019/10/23)
The present invention provides a diclofenac synthetic method, which belongs to the technical field of drug synthesis; synthetic method of this invention the specific reaction steps are as follows: step 1): compound (a) in the presence of sodium methoxide/methanol reaction, to obtain compound (b); step 2): compound (b) with a compound (c) in the presence of an alkali reaction, to obtain compound (d); step 3): compound (d) with a compound (e) in the organic solvent, under the action of catalyst reaction, to obtain compound (f); the method of raw materials are easy, simple operation, high yield, low cost, less wastes, high safety, is suitable for industrial production. (by machine translation)
Metal-Free Tandem Rearrangement/Lactonization: Access to 3,3-Disubstituted Benzofuran-2-(3H)-ones
Santi, Micol,Ould, Darren M. C.,Wenz, Jan,Soltani, Yashar,Melen, Rebecca L.,Wirth, Thomas
, p. 7861 - 7865 (2019/04/25)
A novel metal-free synthesis of 3,3-disubstituted benzofuran-2-(3H)-ones through reacting α-aryl-α-diazoacetates with triarylboranes is presented. Initially, triarylboranes were successfully investigated in α-arylations of α-diazoacetates, however in the presence of a heteroatom in the ortho position, the boron enolate intermediate undergoes an intramolecular rearrangement to form a quaternary center. The intermediate cyclizes to afford valuable 3,3-disubstituted benzofuranones in good yields.
Synthetic method of diclofenac sodium (by machine translation)
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, (2019/01/08)
The invention belongs to the technical field of pharmaceutical chemical synthesis, specific non-steroidal anti-inflammatory analgesic synthetic method of diclofenac sodium. Synthetic method of this invention the reaction steps are as follows: by the phenylacetic acid nitration reaction layer which O-nitrophenyl acetate (2); by the compound (2) by hydrogenation reduction reaction O-amino acetate (3); by the compound (3) amino through amidation, to obtain 2 - (2 - benzamido-phenyl) acetate (4); by the compound (4) with thionyl chloride produce chlorinated imine intermediate, then under the action of the inorganic base with 2, 6 - dichlorophenol condensation preparation (E) - Methyl - 2 - (2 - ((2, 6 - dichloro phenoxy) (phenyl) methylene amino) phenyl) ester (5); by the compound (5) by the Chapman rearrangement reaction for preparing methyl 2 - (2 - (N- (2, 6 - Dichlorophenyl) benzoyl amino) phenyl) ester (6); by the compound (6) by hydrolysis to prepare diclofenac sodium. Benzene acetic acid methyl ester calculation, the overall yield is 67%. The method of the invention raw materials are easy, economic cost, simple operation, mild reaction conditions, the industrial production is easy. (by machine translation)
Enantioselective Synthesis of trans-2,3-Dihydro-1H-indoles Through C–H Insertion of α-Diazocarbonyl Compounds
Santi, Micol,Müller, Simon T. R.,Folgueiras-Amador, Ana A.,Uttry, Alexander,Hellier, Paul,Wirth, Thomas
, p. 1889 - 1893 (2017/04/21)
A stereoselective synthesis of 2,3-dihydro-1H-indoles with a RhII-catalyzed C–H insertion is reported. The α-diazo carbonyl intermediates can be obtained by a diazo-transfer reaction of 2-aminophenylacetic acids. Optimization and kinetic studie
CYCLOPROPANECARBOXAMIDO-SUBSTITUTE AROMATIC COMPOUNDS AS ANTI-TUMOR AGENTS
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, (2015/07/22)
Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
Visible-Light-Induced Meerwein Cascade Reactions for the Preparation of α-Aryl Esters
Niu, Teng-Fei,Li, Liang,Ni, Bang-Qing,Bu, Mei-Jie,Cai, Chun,Jiang, Hui-Liang
, p. 5775 - 5780 (2015/09/15)
A practical strategy has been developed for preparation of α-aryl ester derivatives by using a visible-light-induced Meerwein cascade reaction. This method uses molecular oxygen as an oxidant at room temperature without the need of hazardous reagents or harsh reaction conditions and provides a straightforward approach to pharmaceutically and synthetically useful α-aryl esters in moderate to good yields from simple and readily available starting materials. Oxindoles were also prepared by this protocol. A new strategy for the synthesis of α-aryl esters has been reported. This protocol utilizes acrylonitrile as a "bridge molecule" to combine a visible-light-induced Meerwein reaction and a hydrolysis reaction to generate α-aryl esters. This method was also employed for the preparation of oxindoles.