Tetrahedron

Formal synthesis of TMC-69-6H via a one-pot enantioselective domino proline-mediated aldol/olefin homologation procedure

S Vuong, N Brondel, C Len, S Papot, B Renoux

Index: Vuong, Sophie; Brondel, Nicolas; Len, Christophe; Papot, Sebastien; Renoux, Brigitte Tetrahedron, 2012 , vol. 68, # 2 p. 433 - 439

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Abstract

Recently, 4-hydroxy-2-pyridone-containing alkaloids have emerged as attractive targets in medicinal chemistry. Numerous derivatives of this family exhibit a wide range of biological effects including antibacterial, antifungal, and cytotoxic activities. 1 In 2001, the Kohno group reported the isolation and structural determination of a new antibiotic, 2 TMC-69 1, from the fermentation broth of a mitosporic fungus, Chrysosporium sp. TC 1068 ( Scheme 1). This pyridone showed ...