Total synthesis of rapamycin. Maddess, M., L., Tackett, M., N., Watanabe, H., Brennan, P., E., Spilling, C., D., Scott, J., S., Osborn, D., P., & Ley, S., V. Angewandte Chemie - International Edition, 46(4):591-597, Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
Total synthesis of rapamycin [pdf]Paper  Total synthesis of rapamycin [link]Website  doi  abstract   bibtex   1 download  
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: 1