钯催化的酰胺的直接 C(sp 2 )-H 邻位芳基化反应，使用 2-氨基苯基吡唑作为导向基团。
Palladium-Catalyzed Direct C(sp)-H ortho-Arylation of Anilides Using 2-Aminophenylpyrazole as the Directing Group.
机构信息
Department of Chemistry, University of San Francisco , 2130 Fulton Street, San Francisco, California 94117, United States.
出版信息
J Org Chem. 2017 Nov 3;82(21):11620-11625. doi: 10.1021/acs.joc.7b01883.
Palladium-catalyzed ortho-arylation of anilides was achieved using 2-aminophenyl-1H-pyrazole (2-APP) as a new directing group. Using Pd(OAc) as the catalyst and AgO as the promoter, mono- and diarylation of anilides were realized in up to 89% isolated yield. Further manipulation of the arylation product may be accomplished by a 2-step sequence involving an acidic hydrolysis of the methylated amide. More interestingly, in the presence of KCO, tandem C-C/C-N cyclization products were obtained for a couple of substrates.
钯催化的酰苯胺的邻位芳基化反应，使用 2-氨基苯基-1H-吡唑（2-APP）作为一个新的导向基团。使用 Pd(OAc)2 作为催化剂和 AgO 作为促进剂，实现了酰苯胺的单芳基化和二芳基化，收率高达 89%。通过两步序列，包括对甲酰胺的酸性水解，可以进一步对芳基化产物进行操作。更有趣的是，在 KCO 的存在下，一些底物可以得到 C-C/C-N 串联环化产物。
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