- Synthetic method of non-steroidal antiinflammatory drug pain killing
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The invention discloses a synthesis method of non-steroidal anti-inflammatory drug tolmetin. The methodcomprises the following steps: sequentially preparing a sulfuric acid-containing acetonedicarboxylic acid crude product, 2-(2-acetoxy)-1-methyl-1H-pyrrole-3-formic acid and 2-(2-alkyl acetate)-1-methyl-1H-pyrrole-3-formic acid by taking citric acid or citric acid monohydrate as a raw material; and carrying out decarboxylation, acylation, hydrolysis and acidification to obtain tolmetin. The synthetic method provided by the invention overcomes the defect that the existing tolmetin preparation process depends on N-methylpyrrole, and is a low-cost, low-pollution and high-yield synthetic method of non-steroidal anti-inflammatory drug tolmetin.
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Paragraph 0041; 0048-0049; 0055; 0062-0063; 0094; 0101-0102
(2021/04/17)
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- NOVEL MACROCYCLIC DERIVATIVES, PROCESS FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
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Compound of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, X, Y and G are as defined in the description, and their use in the manufacture of medicaments.
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Paragraph 0362; 0363
(2020/08/25)
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- Synthesis, antimicrobial, and anti-inflammatory activities of acetamido pyrrolyl azoles
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The acetamido pyrrolyl oxazoles/thiazoles/imidazoles were prepared and tested for their antimicrobial and anti-inflammatory activities. The nitro substituted acetamido pyrrolyl thiazole (11f) and pyrrolyl imidazole (12f) exhibited promising antibacterial activity against K. pneumoniae. The compound 12f showed good antifungal activity against P. chrysogenum. The methoxy acetamido pyrrolyl oxazole (10c) displayed potential anti-inflammatory activity.
- Sowmya, Donthamsetty V.,Basha, Shaik Sharafuddin,Devi, Palampalli Uma Maheswari,Lavanyalatha, Yerraguravagari,Padmaja, Adivireddy,Padmavathi, Venkatapuram
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p. 1010 - 1021
(2017/04/13)
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- Synthesis and process optimization of amtolmetin: An antiinflammatory agent
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Efforts toward the synthesis and process optimization of amtolmetin guacil 1 are described. High-yielding electrophilic substitution followed by Wolf-Kishner reduction are the key features in the novel synthesis of tolmetin 2 which is an advanced intermediate of 1.
- Reddy, Lekkala Amarnath,Chakraborty, Saurya,Swapna, Rodda,Bhalerao, Dinesh,Malakondaiah, Golla China,Ravikumar, Mylavarapu,Kumar, Abhijeet,Reddy, Gade Srinivas,Naram, Jyothirmayi,Dwivedi, Namrata,Roy, Arnab,Himabindu, Vurimidi,Babu, Bangaru,Bhattacharya, Apurba,Bandichhor, Rakeshwar
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experimental part
p. 362 - 368
(2011/03/21)
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- Friedel - Crafts acylation of pyrroles and indoles using 1,5-diazabicyclo[4.3.0]non-5-ene (DBN) as a nucleophilic catalyst
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1,5-Diazabicyclo[4.3.0]non-5-ene (DBN) has been shown to be an effective catalyst for the regioselective Friedel - Crafts C-acylation of pyrroles and indoles in high yields. A detailed mechanistic study implies that DBN is acting as a nucleophilic organocatalyst, with the X-ray crystal structure of a key N-acyl-amidine intermediate having been determined for the first time.
- Taylor, James E.,Jones, Matthew D.,Williams, Jonathan M. J.,Bull, Steven D.
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p. 5740 - 5743
(2011/03/18)
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- 1,2-disubstituted-6-oxo-3-phenyl-piperidine-3-carboxamides and combinatorial libraries thereof
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The invention relates to combinatorial libraries containing two or more novel piperidine-3-carboxamide derivative compounds, methods of preparing the piperidine-3-carboxamide derivative compounds and piperidine-3-carboxamide derivative compounds bound to a resin
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- Process for preparing pyrrole-2-acetic acids
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N-H and N-loweralkyl pyrrole-2-acetic acids are prepared by the reduction of 1-H and 1-loweralkyl-α-trichloromethylpyrrole-2-methanol with sodium dithionite (sodium hydrosulfite) in the presence of a base, MOH, wherein M is an alkali metal, an alkaline earth metal or tetraalkyl ammonium.
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- Preparation of pyrrole-2-acetates
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Loweralkyl 1-loweralkyl-pyrrole-2-glyoxylates are reduced by the base-catalyzed action of hydrogen sulfide under pressure of at least 30 p.s.i. to loweralkyl 1-loweralkyl-pyrrole-2-acetates.
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