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叠氮丙烯酰胺的连续流动热解合成杂环和药物中间体。

Continuous flow thermolysis of azidoacrylates for the synthesis of heterocycles and pharmaceutical intermediates.

机构信息

Max Planck Institute of Colloids and Interfaces, Department of Biomolecular Systems, Potsdam, Germany.

出版信息

Chem Commun (Camb). 2011 Mar 7;47(9):2688-90. doi: 10.1039/c0cc04481d. Epub 2010 Dec 20.

Abstract

An efficient, safe and scalable procedure for the continuous flow thermolysis of azidoacrylates to yield indoles has been developed and was applied to the synthesis of related heterocycles. The scalability of the process was demonstrated in the continuous flow synthesis of a precursor to the DAAO inhibitor 4H-furo[3,2-b]pyrrole-5-carboxylic acid.

摘要

已经开发出一种高效、安全且可扩展的连续流动叠氮丙烯酸酯热解方法,用于生成吲哚,并将其应用于相关杂环的合成。该方法的可扩展性在 DAAO 抑制剂 4H-呋喃[3,2-b]吡咯-5-羧酸前体的连续流动合成中得到了证明。

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