4.2 Article

TOTAL SYNTHESIS OF THERMOACTINOAMIDE A AND ITS ANALOGUE

Journal

HETEROCYCLES
Volume 98, Issue 6, Pages 789-797

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.3987/COM-19-14076

Keywords

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Funding

  1. National Natural Science Foundation of China [21602078, 21672084, 81874292]
  2. Science and Technology Planning Project of Guangzhou [201704030042, 201710010088]
  3. National Key Research and Development Plan of China [2018YFC0310900]
  4. Scientific Research Cultivation and Innovation Fund Research Project of Jinan University [21616113, 21617472]
  5. fundamental research funds for the central university

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Thermoactinoamide A, showing remarkable antibacterial properties, is a novel cyclic hexapeptide which was originally isolated from thermophilic bacterium. We disclosed here the first total synthesis of thermoactinoamide A and its analogue, anti-thermoactinoamide A, by the Fmoc solid-phase peptide synthesis and subsequent efficient macrolactamization. Thermoactinoamide A and its analogue can be obtained in 74% and 46% overall yield respectively without any isomerization under the developed methodology.

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