Abstract

AbstractIsoxazolidines and 1,3‐aminoalcohols with a piperazin‐2‐one skeleton were readily prepared on a solid support through [3+2] cycloaddition and subsequent N−O‐bond cleavage, starting from a polymer‐supported cyclic nitrone. Libraries of functionalized 1,3‐aminoalcohols and their derivatives were obtained by automated amine acylation and Mitsunobu reactions on a solid support. The key to success is the oxidation of the immobilized cyclic secondary amine precursor to the nitrone on a solid support and the reductive N−O‐bond cleavage of the isoxazolidines, employing Mo(CO)6. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004)

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