Palladium-Catalyzed sp3 C?H Benzoxylation of Alanine Derivatives Using Aldehydes under Ambient Conditions
Palladium-Catalyzed sp3 C?H Benzoxylation of Alanine Derivatives Using Aldehydes under Ambient Conditions
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常温条件下钯催化的乙醛对丙氨酸衍生物的 sp3 C?H 苯氧基化
DOI：
10.1055/a-1422-9632
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发表时间：
2021
期刊：
影响因子：
--
通讯作者：
Wang Jiarui
中科院分区：
文献类型：
--
作者：
Kanyiva Kyalo Stephen;Shibata Takanori;Tang King Hung Nigel;Wang Jiarui
本文报道了Pd（Ⅱ）催化下，以8-氨基喹啉为导向基团的N-邻苯二甲酰丙氨酸衍生物与醛的sp_3C-H键苯甲酰氧基化反应。当丙氨酸衍生物和醛在甲苯/水共溶剂中的溶液在钯催化剂和叔丁基过氧化氢存在下在室温下反应时，以高达68%的产率形成苄氧基化产物。顺利地除去所得苄氧基化产物的保护基，以高产率得到游离酰胺。
The Pd(II)-catalyzed sp3C–H bond benzoxylation ofN-phthaloylalanine derivatives possessing an 8-aminoquinolyl group as a directing group with aldehydes under ambient conditions is reported. When a solution of an alanine derivative and an aldehyde in a toluene/water co-solvent was reacted in the presence of palladium catalyst andtert-butyl hydroperoxide at room temperature, a benzoxylated product was formed in up to 68% yield. The protecting group of the obtained benzoxylated product was smoothly removed to afford a free amide in high yield.