Indomethacin Synthesis, Historical Overview of Their Structural Modifications

• Published in: ChemistrySelect (Weinheim) 2022-10, Vol.7 (37), p.n/a
• Main Authors: Torres‐Carbajal, Karina R., Segura‐Quezada, Luis A., Ortíz‐Alvarado, Rafael, Chávez‐Rivera, Rubén, Tapia‐Juárez, Melissa, González‐Domínguez, Martha I., Ruiz‐Padilla, Alan J., Zapata‐Morales, Juan R., León‐Solís, Claudia, Solorio Alvarado, César R.
• Format: Article
• Language: English
• Subjects: anti-inflammation; COX-2 selective; Indomethacin
• ISSN: 2365-6549; 2365-6549
• DOI: 10.1002/slct.202201897

One of the most important (NSAID) non‐steroidal anti‐inflammatory drug‐containing the indol core is represented by the indomethacin. This highly relevant compound has been used for the last 50 years with excellent pharmacological results. Due to its relevant efficacy as an anti‐inflammatory treatment, several syntheses have been developed during this half of century. Herein is summarized and discussed the most representative strategies which successfully addressed the total syntheses of indomethacin as well as some of its derivatives generated by carrying out strategic modifications at the nitrogen atom, the carboxylic acid at C‐3, the methoxy group at C‐5 and the methyl group at C‐2. Indomethacin is one of the most important indolic non‐steroidal anti‐inflammatories (NSAID) used along the last 50 years. Different synthesis and key structural modifications on the most important sites of the indole core for increasing its activity which have been carried out to date are herein reviewed.