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A cinchona alkaloid catalyzed asymmetric Mannich reaction of 4-hydroxycoumarins and N-p-tolylsulfinylimines was achieved to synthesize enantioenriched α-benzylaminocoumarins in moderate to excellent yields (up to 99%) and with moderate to good enantioselectivities (up to 83% ee). The absolute configuration of the resulting chiral amines was assigned by analysis of computational and experimental electronic...
A novel one-pot asymmetric synthesis of densely substituted α-methylene-γ-lactams in favor of cis-isomer involving Zn-promoted aza-Barbier-type reaction has been well established. A wide array of α-methylene-γ-lactams were obtained in high yields with excellent diastereomeric ratios from 98:2 to >99:1 and good enantioselectivities. The synthetic potential of such α-methylene-γ-lactams was demonstrated...
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