期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 15, 期 12, 页码 2874-2914出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.200801656
关键词
anticancer agents; immunosuppressive agents; macrocyclization; natural products; total synthesis
资金
- EPSRC [EP/F069685/1] Funding Source: UKRI
- Engineering and Physical Sciences Research Council [EP/F069685/1] Funding Source: researchfish
- Biotechnology and Biological Sciences Research Council Funding Source: Medline
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.
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