Volume 7, Issue 3 (10-2025)
Tabari Biomed Stu Res J 2025, 7(3): 36-45 |
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Siadati S A, Ebrahimzadeh M, Babanezhad E. Synthesis routes from Salicylic acid to Mesalazine; A short Review. Tabari Biomed Stu Res J 2025; 7 (3) :36-45
URL: http://tbsrj.mazums.ac.ir/article-1-3894-en.html
URL: http://tbsrj.mazums.ac.ir/article-1-3894-en.html
Abstract:
This mini-review provides a chronological and mechanistic overview of synthetic developments leading from salicylic acid to mesalazine (5-aminosalicylic acid). Historical nitration routes (1843–1954) relied on mineral acids under uncontrolled conditions, while modern approaches (2005–2025) have achieved regioselective 5-nitration with yields exceeding 85% using catalytic, microwave-assisted, or solvent-free systems. Subsequent reduction of 5-nitrosalicylic acid to its amine derivative has evolved from tin or sulfide reagents to environmentally benign catalytic hydrogenations, electrochemical, and mechanochemical protocols. Recent industrial patents and academic studies demonstrate scalable aqueous hydrogenations with precise pH control and remarkable product selectivity.
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