Total Synthesis of rapamycin. Ley, S., V., Tackett, M., N., Maddess, M., L., Anderson, J., C., Brennan, P., E., Cappi, M., W., Heer, J., P., Helgen, C., Kori, M., Kouklovsky, C., Marsden, S., P., Norman, J., Osborn, D., P., Palomero, M., Á., Pavey, J., B., Pinel, C., Robinson, L., A., Schnaubelt, J., Scott, J., S., Spilling, C., D., Watanabe, H., Wesson, K., E., & Willis, M., C. Chemistry - A European Journal, 15(12):2874-2914, Wiley-VCH Verlag GmbH & Co. KGaA, 2009.
Total Synthesis of rapamycin [pdf]Paper  Total Synthesis of rapamycin [link]Website  doi  abstract   bibtex   
For over 30 years, rapamycin has generated a sustained and intense interest from the scientific community as a result of its exceptional pharmacological properties and challenging structural features. In addition to its well known therapeutic value as a potent immunosuppressive agent, rapamycin and its derivatives have recently gained prominence for the treatment of a wide variety of other human malignancies. Herein we disclose full details of our extensive investigation into the synthesis of rapamycin that culminated in a new and convergent preparation featuring a macro-etherification/catechol-templating strategy for construction of the macrocyclic core of this natural product.

Downloads: 0