An efficient one-step functionalization of FK506 by the thiol–ene click (TEC) reaction is reported. This approach, which enables rapid and quantitative generation of bioactive FK1012 and FK506 derivatives, should facilitate biomedical applications of FK506-coupled molecules and expand the scope of the TEC reaction in natural product semi-synthesis.
Z. Guo, R. Zhang and F. Liang, RSC Adv., 2014, 4, 11400 DOI: 10.1039/C3RA47867J
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