Protecting-group-free synthesis of the bisindolylmaleimide
作者：Yong-Chen Gao, Yu-Hui Jia, Ting-Ting Li, Ze-Huan Hei, Feng-Ling Yang, Mu-Hua Huang*, Yun-Jun Luo*
關鍵字：PKC inhibitors, bisindolylmaleimide, GF109203X, arcyriarubin A, protecting groupfree synthesis
論文來源：期刊
具體來源：ARKIVOC
發表時間：2015年
The bisindolylmaleimide GF109203X is a highly selective inhibitor to Protein Kinase C (PKC)
and has attracted much attention. However, its reported synthesis required protecting groups. In order to achieve a short and N-protecting-group-free synthesis of GF109203X, an investigation on N-alkylation of arcyriarubin A was carried out using different bases, solvents and equivalents of bromododecane. It is found that mono-N-alkylation and mono-N''''-alkylation could be achieved respectively. Thus, a protecting-group-free synthesis of GF109203X was accomplished in 40% overall yield starting from indole. This work will lead to a short synthesis of mono-N''''-alkylated arcyriarubins to accelerate drug discovery.