NOVEL SOLUTION-PHASE AND SOLID-PHASE STRATEGIES FOR THE PARALLEL AND COMBINATORIAL SYNTHESIS OF SMALL-MOLECULAR-WEIGHT COMPOUND LIBRARIES

In this account dedicated to '100 years Roche' in CHIMIA, we present s ome of our strategies towards the synthesis of interesting novel amino -acid-derived building blocks; multigeneration synthesis of thiazole l ibraries in solution; a novel solid-phase approach towards highly subs tituted 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 ch emistry combined with a novel cyclization and cleavage strategy, and f inally a novel solid-phase diketopiperazine synthesis combining the Ug i four-component reaction with a final ring-forming cleavage step.