CuI/CuBr₂-catalyzed decarboxylative/A³ reaction of propiolic acids for the facile synthesis of 1,4-diheterocycle-2-butynes

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• 作者：Huangdi Feng ; Panfeng Zhao ; Zhihua Sun ; ^{sungaris@gmail.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：1 ; 4-Diheterocycle-2-butynes ; Decarboxylative coupling ; A3 reaction ; Copper catalyst
• 刊名：Tetrahedron Letters
• 出版年：2015
• 出版时间：7 October 2015
• 年：2015
• 卷：56
• 期：41
• 页码：5676-5680
• 全文大小：2690 K

文摘

A novel and efficient microwave-assisted protocol to 1,4-diheterocycle-2-butynes was successfully developed. The method is based on one-pot copper-catalyzed A³ reaction/decarboxylative coupling of a propiolic acid, a formaldehyde, and a 1,2- or 1,3-amino alcohol. This multicomponent coupling reaction provides a straight forward access to introduction oxazolidine or 1,3-oxazinane at the 1,4-position of a but-2-yne from readily available starting materials. 1,4-Diheterocycle-2-butynes with diverse substitution patterns are obtained in moderate to good yields.