A Route to Azafluoranthene Natural Products Through Direct Arylation

Microwave‐assisted direct arylation reactions were successfully employed in the synthesis of azafluoranthene alkaloids for the first time. Direct arylation reactions on a diverse set of phenyltetrahydroisoquinolines produces the indeno[1,2,3‐ ij ]isoquinoline nucleus required towards a high‐yielding azafluoranthene synthesis. The method was used as a key step in the efficient preparation of the natural products rufescine and triclisine. As demonstrated herein, this synthetic approach should be generally applicable to the preparation of natural and un‐natural azafluoranthene alkaloids as well as azafluoranthene‐like isoquinoline alkaloids.