Synthesis, asymmetric diversity orientated

Multicomponent reactions (MCRs) are one-pot processes combining three or more substrates simultaneously [1], MCR processes are of great interest, not only because of their atom economy but also for their application in diversity-oriented synthesis and in preparing libraries for the screening of functional molecules. Catalytic asymmetric multicomponent processes are particularly valuable but demanding and only a few examples have been realized so far. Here we provide an overview of this exciting and rapidly growing area. 

Stavenger, R.A. and Schreiber, S.L., Asymmetric catalysis in diversity-oriented organic synthesis enantioselective synthesis of 4320 encoded and spatially segregated dihydropyrancarboxamides, Angew. Chem., Int. Ed. Engl., 40, 3417, 2001. 

Reaction control in the organocatalytic asymmetric one-pot, three-component reaction of aldehydes, diethyl a-aminomalonate and nitroalkenes toward diversity-oriented synthesis. 

And indeed, the three compounds showed cytotoxicity in the low micromolar range. This example nicely demonstrates the force of asymmetric MCRs in the diversity-oriented synthesis and drug discovery. 

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