Applications of MCRs to Process Development

Molecules containing this substituted piperazine core are important pharmacophores (particularly for GPCR related ligands) and have been reported in several drugs under development [95]. Scientists at Merck recently introduced a novel one-pot isocyanide-based MCR affording the desired substituted piperazine, reportedly compatible with array synthesis. 

3 Armstrong, R. W. Brown, S. D. Keating, T. A. Tempest, P. A. Combinatorial Chemistry. Synthesis and Application-, Wilson, S. R. Czarnik, A. W., eds. John Wiley Sons, New York, 1997, pp. 153-190. 

25 (a) Note when dealing with low molecular weight isocyanides, it is advisable to wash all glassware in methanolic/HCl solutions to convert the reagent to its corresponding hydrated and non-pungent forma-mide. (b) Note one exception to the low toxicity rule is diisocyanobutane 

33 Semple, J. E. Passerini reaction revisited 034, MCR2003, April 11-14, 2003, Genoa, Italy. 

35 Jones, W. Tadesse, S. Chenera, B. Viswanadhan, V. Hulme, C. A.C.S, 223rd, American Chemical Society Meeting and Exposition, April 2002, New Orleans, LA. 

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