Pharmaron (Ningbo) Technology Development Co., Ltd., No. 800 Bin-Hai fourth Road, Hangzhou Bay New Zone, Ningbo 315336, P. R. China.
Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China.
Org Lett. 2024 Mar 1;26(8):1688-1693. doi: 10.1021/acs.orglett.4c00187. Epub 2024 Feb 22.
Using a novel homologation-heterocyclization cascade, the on-DNA synthesis of benzofurans from aldehydes has been developed. The methodology, based on an innovative use of the Seyferth-Gilbert homologation, followed by a high yielding Sonogashira coupling in situ intramolecular cyclization one-pot, two-step reaction, provides a powerful and unique pathway for DNA-encoded library (DEL) synthesis of a wide array of pharmaceutically relevant benzofuran-based scaffolds.
采用一种新颖的同系化-杂环化级联反应，从醛类化合物在 DNA 上合成苯并呋喃。该方法基于对 Seyferth-Gilbert 同系化的创新应用，随后进行高产 Sonogashira 偶联的原位分子内环化一锅两步反应，为基于 DNA 编码文库（DEL）的广泛的具有药物相关性的苯并呋喃骨架提供了一种强大而独特的合成途径。
