Bakuchiol is an emblematic meroterpene class of natural product extracted from Psoralea corylifolia. It has been reported to possess a broad range of biological and pharmacological properties and is considered as a leading biomolecule. It is highly desirable to devise an efficient approach to access bakuchiol and its chemical biology applications. In this review we provided structural features, isolation methods, various chemical routes and late-stage functionalization (LSF) approaches for bakuchiol and its derivatives. Moreover, this review encompasses the structure–activity relationships (SAR), value-added contributions and future perspectives of bakuchiol