51856-79-2Relevant articles and documents
Synthetic method of non-steroidal antiinflammatory drug pain killing
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Paragraph 0041; 0048-0049; 0055; 0062-0063; 0094; 0101-0102, (2021/04/17)
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.
Synthesis, antimicrobial, and anti-inflammatory activities of acetamido pyrrolyl azoles
Sowmya, Donthamsetty V.,Basha, Shaik Sharafuddin,Devi, Palampalli Uma Maheswari,Lavanyalatha, Yerraguravagari,Padmaja, Adivireddy,Padmavathi, Venkatapuram
, p. 1010 - 1021 (2017/04/13)
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.
Friedel - Crafts acylation of pyrroles and indoles using 1,5-diazabicyclo[4.3.0]non-5-ene (DBN) as a nucleophilic catalyst
Taylor, James E.,Jones, Matthew D.,Williams, Jonathan M. J.,Bull, Steven D.
, p. 5740 - 5743 (2011/03/18)
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.