Synthesis and reactivity of 4-(trifluoromethyl)azetidin-2-ones

Because of the beneficial effect of a trifluoromethyl group on the biological properties of bioactive compounds on the one hand and the versatile synthetic potential of beta-lactams on the other hand, 4-CF3-beta-lactams comprises interesting entities for the preparation of a large variety of CF3-substituted nitrogen-containing target structures with promising biological characteristics. In this review, we present an overview of different building block approach-based routes toward the synthesis of 4-(trifluoromethyl)azetidin-2-ones and the application of the "beta-lactam synthon method" for the synthesis of a diverse set of (a)cyclic CF3-substituted molecules by means of ring-opening and ring-transformation reactions