Abstract: The thesis entitled “ Synthetic studies towards Bulgarein : A naturally occurring Topoisomerase inhibitor” contain three chapters. Bulgarein Chapter 1 deals with brief description of Topoisomerase , their mechanism during DNA replication, transcription, recombination, repairs and their types. An application of Topoisomerase as a target for anticancer chemotherapy i.e. Topoisomerase inhibitor. Chapter 2 describes synthetic studies towards Bulgarein, which divided into two subparts. First part contain intramolecular C-C cross coupling reaction via methodologies like, bioinspired organocatalyzed benzoin condensation, intramolecular pinacol coupling, and intramolecular McMurry condensation. Where, second part describes three thematic methodologies like, directed ortho metalation (DoM), Suzuki cross coupling, and base catalyzed anionic cyclization. Chapter 3 describes, an experimental details for the synthesis of Bulgarein.