Zolimidine, branded as ‘Solimidin’ is a gastroprotective drug based on imidazo[1,2-a] pyridine (imidazo[1,2-a]pyridine) nucleus. The limited synthetic protocols of zolimidine include C–S bond formation, C–N bond formation via C–H activation, S–O bond formation and subsequent derivatization, dehydrogenative heteroannulation, Ortoleva-King-type synthesis, dehydrogenative cyclocondensation, one-pot synthesis reactions, oxidative cross-coupling reactions, and oxidative cyclocondensation. In most of the cases for the synthesis of zolimidine, the formation of parent imidazo[1,2-a] pyridine ring occurs via (using) metal-based catalysts followed by its subsequent functionalization. The therapeutic efficacy of zolimidine as confirmed by its clinical evaluation makes it highly desirable to develop the drug analogs for the critical appraisal and improvement of drug pharmacokinetics and metabolism. In this review, we have discussed the various synthetic strategies aimed at the synthesis of zolimidine, and their chemistry thereof.