钯催化的水相苄醇的苄位 C-H 酰胺化反应：构建喹唑啉酮的策略。
Pd-catalyzed benzylic C-H amidation with benzyl alcohols in water: a strategy to construct quinazolinones.
机构信息
Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan.
出版信息
J Org Chem. 2012 Aug 17;77(16):7046-51. doi: 10.1021/jo301282n. Epub 2012 Aug 9.
PMID:22852777
Abstract
A novel method for the synthesis of 4-phenylquinazolinones via a palladium-catalyzed domino reaction of o-aminobenzamides with benzyl alcohols is developed. This protocol involves N-benzylation, benzylic C-H amidation, and dehydrogenation in water, which may play an important role in the smooth generation of the (η(3)-benzyl)palladium species by activation of the hydroxyl group of the benzyl alcohol.
摘要
开发了一种通过钯催化邻氨基苯甲酰胺与苄醇的级联反应合成 4-苯基喹唑啉酮的新方法。该方案涉及在水中进行 N-苄基化、苄基 C-H 酰胺化和脱氢反应，这可能在通过苄醇的羟基活化生成（η(3)-苄基）钯物种方面发挥重要作用。
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