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synthesis of the key precursor of hirsutellide a合成前体的hirsutellide的关键
Molecules 2005, 10, 259-264
molecules
ISSN 1420-3049
Synthesis of the Key Precursor of Hirsutellide A
1 1 1 1 1 2
Yanjie Xu , Xuemin Duan , Meiling Li , Liqin Jiang , Guangle Zhao , Yi Meng and Ligong
Chen 1,*
1 College of Pharmaceuticals and Biotechnology, Tianjin University, Tianjin, 300072, P.R. China
2 Shenzhen Graduate School of Peking University, Shenzhen University Town, Shenzhen, 518055,
P.R. China
* Author to whom correspondence should be addressed; Email: lgchen@; Telephone:
(+86)-22 Fax: (+86)-22
Received: 27 February 2004 / Accepted: 19 March 2004 / Published: 31 January 2005
__________________________________________________________________________________
Abstract: Hexadepsipeptide 2, the precursor of Hirsutellide A (1), was synthesized in an
overall yield of 45% from N-Boc-Me-Gly via three coupling reactions using
dicyclohexylcarbodiimide (DCC), O-(7-azabenzotriazol-1-yl)-N,N,N’,N’-tetramethyl-
uronium hexafluorophosphate (HATU) and bis(2-oxo-3-oxazolidinyl)phosphinic chloride
(BOP-Cl), respectively.
Keywords: Hirsutellide A, linear hexadepsipeptide, coupled reagent, diazotization
hydrolysis, Boc protection
__________________________________________________________________________________
Introduction
Hirsutellide A (1) is a new antimycobacterial cyclohexadepsipeptide from the cell extracts of
Hirsutella kobayasii BCC 1660. It exhibited anti
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