Rhodium-Catalyzed Annulation of Primary Benzylamine with α-Diazo Ketone toward Isoquinoline

Rhodium-catalyzed annulation of commercially available primary benzylamine with α-diazo ketone was developed, leading to isoquinolines in moderate to good yields. This procedure features the employment of primary benzylamine as starting material as well as high selectivity in the 3- and 4- position of isoquinoline, generating a key compliment to the previously developed annulation with internal alkyne.