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Total synthesis of rapamycin

Authors :
Miles N. Tackett
John B. J. Pavey
Kieron E. Wesson
David Osborn
Maria A. Palomero
Masakuni Kori
Michael C. Willis
James S. Scott
Jag Paul Heer
Matthew L. Maddess
James C. Anderson
Hidenori Watanabe
Paul Brennan
Michael W. Cappi
Catherine Pinel
Joanne Norman
Céline Helgen
Jiirgen Schnaubelt
Stephen P. Marsden
Lesley A. Robinson
Christopher D. Spilling
Steven V. Ley
Cyrille Kouklovsky
Publication Year :
2016

Abstract

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.

Details

Language :
English
Database :
OpenAIRE
Accession number :
edsair.doi.dedup.....54706266323cc943ab83a92c095d5f77