Synthesis and Cytostatic Activity of 14β,15β-Oxazino and 14β,15β-Pyrrolidino Estradiol Derivatives

Highly regioselective synthesis of lactamsviacascade reaction of α,β-unsaturated ketones, ketoamides, and DBU as a catalyst

“…4,5 Lactams and bicyclic lactams were privileged scaffolds presented in numerous natural products and pharmaceuticals. 6 It is signicant to develop new synthesis pathways to construct Lactams and bicyclic lactams with high regioselectivity and high atom-economical by cascade reaction. a,b-Unsaturated ketone is one of most important potential synthons in natural products synthesis [7][8][9][10][11] and have multiple activation sites [12][13][14][15] (a ′ , a, b, g, g ′ Fig.…”

“…Numerous natural products and pharmacologically active compounds contain the structure of the bicyclic lactams with cyclopentanone scaffold, showing the importance of this structural motif in synthetic organic chemistry. 6 Based on our previous research on ketoamides, 48,49 herein, we presented a novel high region-, diastereoselective and atom economical to synthesis of bicyclic lactams via the cascade reaction of aldol-Michael addition on the b and g-positions of cyclopentenone with ketoamides by DBU catalyzed (Scheme 1).…”