Novel Solution- and Solid-Phase Strategies for the Parallel and Combinatorial Synthesis of Small-Molecular-Weight Compound Libraries


  • Alexander Chucholowski
  • Thierry Masquelin
  • Daniel Obrecht
  • Josef Stadlwieser
  • José M. Villalgordo



In this account dedicated to '100 years Roche' in CHIMIA, we present some of our strategies towards the synthesis of interesting novel amino-acid-derived building blocks; multigeneration synthesis of thiazole libraries in solution; a novel solid-phase approach towards highly substituted pyrimidines using a novel safety-catch linker principle and a multidirectional cleavage procedure; a versatile solid-phase synthesis of quinazolones taking advantage of the Staudinger phosphorylimine chemistry combined with a novel cyclization and cleavage strategy, and finally a novel solid-phase diketopiperazine synthesis combining the Ugi four-component reaction with a final ring-forming cleavage step.




How to Cite

A. Chucholowski, T. Masquelin, D. Obrecht, J. Stadlwieser, J. M. Villalgordo, Chimia 1996, 50, 525, DOI: 10.2533/chimia.1996.525.