[en] 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 β-lactams on the other hand, 4-CF₃-β-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 “β-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. Graphical abstract: .

[en] A small set of structurally different monocarbonyl curcuminoids was prepared and screened for cytotoxic activity. In particular, bis-3-methoxy-4-hydroxy- and bis-4-methoxyphenyl-substituted monocarbonyls were synthesized and transformed into the corresponding three-dimensional N-acetylpyrazoline derivatives. In addition, a non-symmetrical indole-based monocarbonyl curcumin was prepared as well. Preliminary cytotoxic evaluation revealed significant effects for 4-hydroxy (pyrazoline) monocarbonyl curcuminoids, whereas the non-phenolic variants displayed rather poor activity. Graphic abstract:

.