细胞三烯菌素大环核心的汇聚合成：RCM在大环化中的应用。

A convergent synthesis of the macrocyclic core of cytotrienins: application of RCM for macrocyclization.

作者信息

Evano Gwilherm, Schaus Jennifer V, Panek James S

机构信息

Department of Chemistry and Center for Chemical Methodology and Library Development, Boston University, 590 Commonwealth Avenue, Boston, Massachusetts 02215, USA.

出版信息

Org Lett. 2004 Feb 19;6(4):525-8. doi: 10.1021/ol036284k.

DOI:10.1021/ol036284k

PMID:14961614

Abstract

[reaction: see text] The asymmetric synthesis of the fully elaborated macrocyclic core of cytotrienins A-D, potent apoptosis-inducing agents, is described. Synthetic highlights include the construction of the aniline bond using a copper-mediated amidation and the use of a ring-closing metathesis (RCM) reaction to efficiently install the (E,E,E)-triene and simultaneously construct the macrocyclic lactam.

摘要

[反应：见正文] 描述了细胞三烯素A-D（强效凋亡诱导剂）完全合成的大环核心的不对称合成。合成亮点包括使用铜介导的酰胺化反应构建苯胺键，以及使用闭环复分解（RCM）反应高效地安装（E,E,E）-三烯并同时构建大环内酰胺。