Pyridazino [4,5-b]indole is an important class of heterocyclic compounds with numerous applications in the field of medicinal chemistry. This review summarizes the synthetic methods of pyridazino [4,5-b]indoles published during the period from 1962 to 2022. In this review, we have discussed different methods for the synthesis of pyridazino [4,5-b]indole from various starting materials and the difficulties that scientists faced during the preparation process. We focus on the recent developments in synthetic methods of the pyridazino [4,5-b]indoles. Pyridazino[4,5-b]indoles Biological importance of pyridazino[4,5-b]indoles ✓ As anxiolytic ✓ As antihypertensive ✓ As thromboxane A2 synthetase inhibitors ✓ As antihistaminic ✓ As HIV-1 reverse transcriptase inhibitors ✓ As antiarrhythmics ✓ As phosphatidylinositol 3-kinase (PI3K) inhibitors ✓ As blood platelet aggregation inhibitors