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Publication 48  

  1. Modular Synthesis of Radicicol A and Related Resorcylic Acid Lactones, Potent Kinase Inhibitors
    P.-Y. Dakas, S. Barluenga, F. Totzke, U. Zirrgiebel, N. Winssinger
    Angew. Chem. Int. Ed. 2007, 46, 6899-6902

Short and sweet: A concise and modular synthesis of radicicol A and related resorcylic acid lactones using fluorous isolation technology and immobilized reagents is reported (see scheme, RF=C3H6C6F13, TMSE=2-(trimethylsilyl)ethyl). The compounds are found to be potent (low-nanomolar) inhibitors of selected kinases. Despite their irreversible inactivation of kinases, they show good selectivity amongst a panel of 127 kinases.

DOI: 10.1002/anie.200702406 

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