Synthesis of 3-Substituted and 2,3-Disubstituted Quinazolinones via Cu-Catalyzed Aryl Amidation

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• 作者：Lanting Xu ; Yongwen Jiang ; Dawei Ma
• 刊名：Organic Letters
• 出版年：2012
• 出版时间：February 17, 2012
• 年：2012
• 卷：14
• 期：4
• 页码：1150-1153
• 全文大小：330K
• 年卷期：v.14,no.4(February 17, 2012)
• ISSN：1523-7052

文摘

CuI/4-hydroxy-l-proline catalyzed coupling of N-substituted o-bromobenzamides with formamide takes place at 80 掳C, affording 3-substituted quinazolinones directly. Under these conditions other amides that were tested only provided simple coupling products, which can be converted into 2,3-disubstituted quinazolinones via HMDS/ZnCl₂ mediated condensative cyclization.