Thiourea is an important building block found in several drug molecules such as thioacetazone, enzalutamide, thiocarlide etc. Thiourea derivatives have been used for activation of carbonyl and imine compounds to facilitate Michael addition reactions, and as an oxyanion stabilizer for [Ir] catalyzed amination of alcohols without using any base or acid. Chiral bifunctional thiourea catalysts have been successfully applied for asymmetric synthesis of several drug molecules.