通过连续大环化和环间芳构化全合成 TAK 激酶抑制剂 LL-Z1640-2。
Total synthesis of TAK-kinase inhibitor LL-Z1640-2 via consecutive macrocyclization and transannular aromatization.
机构信息
Department of Chemistry, Imperial College, London SW7 2AZ, England.
出版信息
Org Lett. 2010 Dec 3;12(23):5573-5. doi: 10.1021/ol102468k. Epub 2010 Nov 10.
PMID:21067221
Abstract
The biomimetic total synthesis of LL-Z1640-2 (3) is reported without the use of phenol protection. The aromatic unit was constructed via the transannular aromatization of macrocyclic triketo-ester 2, which in turn was synthesized by macrolactonization using an intramolecular trapping of a triketo-ketene derived from dioxinone 1.
摘要
本文报道了无需使用苯酚保护基的 LL-Z1640-2（3）的仿生全合成。通过大环三酮酯 2 的环间芳构化构建芳环单元，大环内酯化则使用二恶英酮 1 衍生的三酮-烯酮的分子内捕获来合成 2。
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