Copper-catalyzed annulation of α-substituted diazoacetates with 2-ethynylanilines: the direct synthesis of C2-functionalized indoles.
Copper-catalyzed direct annulation of α-substituted diazoacetates with 2-ethynylanilines leading to C2-functionalized indoles was achieved under mild reaction conditions. The C2-(carboxylate methyl) substituted indoles were obtained in moderate to high yields. In addition, this procedure tolerates a series of N-substituted and free substituted 2-ethynylanilines.
School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, P. R. China. jtsun08@gmail.com.
Gang
G
Liu
Guangyang
G
Xu
Jian
J
Li
Dong
D
Ding
Jiangtao
J
Sun
D000085:Acetates / Q000737:chemistry*; D000114:Acetylene / Q000031:analogs & derivatives* / Q000737:chemistry; D000814:Aniline Compounds / Q000737:chemistry*; D002384:Catalysis; D003300:Copper / Q000737:chemistry*; D003979:Diazonium Compounds / Q000737:chemistry*; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000737:chemistry*
C483919:2-ethynylaniline; D000085:Acetates; D000814:Aniline Compounds; D003979:Diazonium Compounds; D007211:Indoles; D009942:Organometallic Compounds; D003300:Copper; D000114:Acetylene