Synfacts 2007(5): 0457-0457  
DOI: 10.1055/s-2007-968392
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of Antibiotic GE2270A

Contributor(s):Philip Kocienski
K. C. Nicolaou*, B. Zou, D. H. Dethe, D. B. Li, D. Y.-K. Chen
Agency for Science, Technology, and Research, Singapore; The Scripps Research Institute and University of California, San Diego, La Jolla, USA
Total Synthesis of Antibiotics GE2270A and GE2270T
Angew. Chem. Int. Ed.  2006,  45:  7786-7792  
Further Information

Publication History

Publication Date:
24 April 2007 (online)


Significance

G2270A is a thiopeptide antibiotic isolated from Planobispora rosea that inhibits bacterial elongation factor Tu but not the eukaryote elongation factor-1 alpha. The key step entails a hetero-Diels-Alder dimerization to generate the pyridine scaffold (red).

Comment

The hetero-Diels-Alder reaction used to construct the pyridine core was previously used in a synthesis of thiostreptone (K. C. Nicolaou et al. J. Am. Chem. Soc. 2005, 127, 11159-11175).