Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida, Sakyo-ku, Kyoto 606-8501, Japan.
Org Lett. 2012 Aug 17;14(16):4270-3. doi: 10.1021/ol302035j. Epub 2012 Jul 31.
Synthesis of the indole skeleton was achieved using a Pd-catalyzed cascade process consisting of isocyanide insertion and benzylic C(sp(3))-H activation. It was found that slow addition of isocyanide is effective for reducing the amount of catalyst needed and Ad(2)P(n)Bu is a good ligand for C(sp(3))-H activation. The construction of the tetracyclic carbazole skeleton was also achieved by a Pd-catalyzed domino reaction incorporating alkyne insertion.
吲哚骨架的合成就采用了钯催化的级联过程，包括异氰化物插入和苄基 C(sp(3))-H 活化。研究发现，缓慢加入异氰化物可以有效地减少所需催化剂的用量，并且 Ad(2)P(n)Bu 是 C(sp(3))-H 活化的良好配体。四环咔唑骨架的构建也通过钯催化的串联反应实现，其中包括炔烃插入。
