A new indole-tolerant oxidation condition for the synthesis of 1,2-diketone derivatives from the corresponding 1,2-diarylalkynes was described. By screening a series of oxidation systems on alkynes linked with indole and different substituted aromatic ring, the DMSO/PdCl2/CuCl2 system afforded moderate to good yields despite the existence of electron-rich indole ring.
CHENG Xu LI Xiaolong WAN Weili HAO Wenmei HAI Li WU Yong
A new synthetic route of almotriptan was described. The application of Negishi coupling reaction simpli- fied the process and significantly improved the yield. The synthetic route was also expected to be general for the synthesis of other tryptamines like sumatriptan and avitriptan.
LI Xiaolong QIU Rui WAN Weili CHENG Xu HE Yi HAI Li WUYong
