钯催化的 4-苯并呋喃炔酸酯的分子内氢芳基化反应。新型当归素衍生物的合成方法。
Palladium-catalyzed intramolecular hydroarylation of 4-benzofuranyl alkynoates. Approach to angelicin derivatives.
机构信息
Department of Chemistry and Applied Chemistry, Graduate School of Science and Engineering, Saga University, Honjo-machi, Saga 840-8502, Japan.
出版信息
J Org Chem. 2012 Mar 16;77(6):2978-82. doi: 10.1021/jo300021a. Epub 2012 Feb 28.
PMID:22372387
Abstract
Intramolecular hydroarylation of 4-benzofuranyl alkynoates using Pd(OAc)(2) as catalyst took place selectively and efficiently, giving angular furocoumarin derivatives in high yields. The parent angelicin was obtained in 80% yield by this method. The starting 4-benzofuranyl alkynoates were easily accessible from readily available 4-hydroxybenzofurans and alkynoic acids.
摘要
用 Pd(OAc)(2) 作为催化剂，4-苯并呋喃基炔酸酯发生分子内的氢芳基化反应，高效、高选择性地得到角型呋喃香豆素衍生物。该方法以 80%的收率得到了母体花椒毒素。起始的 4-苯并呋喃基炔酸酯可由易得的 4-羟基苯并呋喃和炔酸很容易得到。
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