Synthesis routes from Salicylic acid to Mesalazine; A short Review

This mini-review provides a chronological and mechanistic overview of synthetic developments leading from salicylic acid to mesalazine (۵-aminosalicylic acid). Historical nitration routes (۱۸۴۳–۱۹۵۴) relied on mineral acids under uncontrolled conditions, while modern approaches (۲۰۰۵–۲۰۲۵) have achieved regioselective ۵-nitration with yields exceeding ۸۵% using catalytic, microwave-assisted, or solvent-free systems. Subsequent reduction of ۵-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.

کلیدواژه ها:

Mesalazine ، Salicylic acid ، ۵-Nitration ، Nitro reduction ، Green chemistry