In this study, indobufen was successfully synthesized from diludine triggered metal-free cascade in good yield. This process includes esterification, reduction, reductive amination/ condensation cascade, hydrolysis and recrystallization. Additionally, the post-treatment procedure was greatly simplified, and indobufen can be obtained by simple recrystallization that complies with the pharmacopoeia standards. Moreover, this work will be used as a basis for further research into the efficient production of indobufen on an industrial scale.