In this paper, we report an efficient and versatile methodology for the synthesis of a series of novel heteroaryl‐1,2,3‐triazoles connected to 4‐methylcoumarin (4‐methyl‐2H‐chromen‐2‐one) via oxymethylene linker. The desired molecules were accessed by both two‐step synthesis and the one‐pot copper catalyzed cycloaddition reaction of heteroaromatic azides with coumarin containing acetylenes. The developed protocol was found to be facile and effective for preparing a series of novel heteroaryl‐1,2,3‐triazole‐coumarin conjugates in excellent yields. Practical utility of one‐pot protocol has been confirmed by the successful gram‐scale synthesis of 1,3‐Dimethyl‐6‐(4‐[([4‐methyl‐2‐oxo‐2H‐chromen‐7‐yl]oxy)methyl]‐1H‐1,2,3‐triazol‐1‐yl)pyrimidine‐2,4(1H,3H)‐dione.

中文翻译：

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通过醚连接基连接到香豆素的1-杂芳基-1,2,3-三唑的设计与合成

在本文中，我们报告了一种高效且通用的方法，用于合成一系列通过甲醛连接基连接到4-甲基香豆素（4-甲基-2H-铬-2--2-酮）的杂芳基-1,2,3-三唑。通过两步合成以及杂芳族叠氮化物与含有乙炔的香豆素的一锅铜催化的环加成反应，均可获得所需的分子。已发现开发的方案既容易又有效，可以以高收率制备一系列新型杂芳基-1,2,3-三唑-香豆素共轭物。成功地通过克级合成1,3-二甲基-6-（4-[（[[4-甲基-2-氧代-2H-铬--7-基]氧基]一锅法证实了一锅法的实用性甲基] -1H-1,1,2,3-三唑-1-基）嘧啶-2,4（1H，3H）-二酮。