Abstract
Abstract1,4‐diamino‐2‐butynes are important structural motifs in biologically active molecules, however, their synthesis with high selectivity remains a challenge. Herein, we develop an effective and straightforward strategy for the modular synthesis of unsymmetrical 1,4‐diamino‐2‐butynes with a high chemoselectivity. This transformation involves a cascade process of copper‐catalyzed decarboxylative A3‐coupling, Petasis reaction, and A3‐coupling, providing a rapid route for synthesizing various target products with broadly functional tolerance and up to 76% yield.
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