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Synlett 1997; 1997(3): 325-326
DOI: 10.1055/s-1997-769
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Combinatorial Synthesis of C(2), C(3)-Disubstituted 3-Hydroxypropionamides Utilizing Baylis-Hillman Reactions on Solid Support

O. Prien, K. Rölfing, M. Thiel, H. Künzer*
  • *Research Laboratories, Schering AG-Berlin, Müllerstr. 170-178, D-13342 Berlin, Germany
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Publication Date:
31 December 2000 (online)

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A four-step reaction protocol for multiple polymer-supported synthesis of structurally diverse α,β-disubstituted 3-hydroxypropionamides 10 has been developed. Variable building blocks were recruited from three monomer pools: primary/secondary amines and aryl aldehydes, the latter of which underwent incorporation into target molecules via Baylis-Hillman reactions. The potential of our approach is demonstrated by machine-assisted assemblage of a small prototype library.

multi-step solid-phase synthesis - combinatorial chemistry - Baylis-Hillman reaction - robot-assisted synthesis