Background: We report a novel MCR4 useful for generating chiral analogs of
staurosporine a promiscuous and potent protein kinases inhibitor.
Method: Our strategy introduces the use of substituted tetramic acids as chiral precursors
which together with an aldehyde, an isocyanide, a dienophile and a Lewis acid lead to
hexa-substituted benzenes in one pot.
Conclusion: Interestingly, the use of chiral precursors not only allowed obtaining a stereo-
controlled reaction, but also observing unusual atropo-diastereomers with axial chirality.
The reaction can be carried out both under thermal or microwave conditions. The
methodology is demonstrated for a panel of aldehydes, tetramic acids, isocyanides and