School of Pharmacy , Sungkyunkwan University , Suwon 16419 , Republic of Korea.
Graduate School of Medicine, Dentistry and Pharmaceutical Science , Okayama University , Okayama 700-8530 , Japan.
J Org Chem. 2018 Apr 20;83(8):4641-4649. doi: 10.1021/acs.joc.8b00388. Epub 2018 Apr 6.
The ruthenium(II)-catalyzed C-H aminocarbonylation of N-(hetero)aryl-7-azaindoles with isocyanates is described. The excellent site selectivity at the ortho-position within the N-(hetero)aryl ring was observed to provide ortho-amidated N-(hetero)aryl-7-azaindoles under the mild reaction conditions. The resulting 7-azaindole derivatives can be readily transformed into 7-azaindoles containing carboxylic acid and alkyl amine functional groups.
报道了钌（II）催化的 N-(杂)芳基-7-氮杂吲哚与异氰酸酯的 C-H 氨甲酰化反应。在温和的反应条件下，观察到在 N-(杂)芳基环的邻位具有优异的位点选择性，从而提供了邻位酰胺化的 N-(杂)芳基-7-氮杂吲哚。所得的 7-氮杂吲哚衍生物可以很容易地转化为含有羧酸和烷基胺官能团的 7-氮杂吲哚。
