向着卢森塔明 A 的全合成迈进：8-表卢森塔明 A 的全合成与生物评价。
Progress toward the total synthesis of lucentamycin A: total synthesis and biological evaluation of 8-epi-lucentamycin A.
机构信息
Department of Chemistry, Vanderbilt University, Nashville, Tennessee 37232, USA.
出版信息
J Org Chem. 2009 Nov 20;74(22):8852-5. doi: 10.1021/jo902115s.
PMID:19908916
Abstract
Synthetic efforts toward the cytotoxic peptides lucentamycins A-D are described that resulted in the total synthesis and biological evaluation of 8-epi-lucentamycin A in 15 steps with 2.2% overall yield. The key epi-nonproteogenic 3-methyl-4-ethylideneproline was synthesized via a titanium-mediated cycloisomerization reaction.
摘要
本文描述了针对细胞毒性肽 Lucentamycins A-D 的合成研究，通过 15 步反应以 2.2%的总收率实现了 8-epi-Lucentamycin A 的全合成，并对其进行了生物评价。关键的非天然的 epino-3-甲基-4-亚乙基脯氨酸通过钛介导的环化异构化反应合成。
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