Abstract
AbstractA mild and metal‐free method for the one‐pot synthesis of highly substituted tetrahydro‐α‐carbolines from Morita‐Baylis‐Hillman (MBH) bromides of nitroalkenes and iminoindolines has been demonstrated. Cascade reaction of MBH bromides with tosyliminoindolines occurs with regio‐ as well as diastereoselectivity in a formal [3+3] manner to form various tetrahydro‐α‐carbolines with wide substrate scope under mild conditions. All the products were obtained in high yields within a short reaction time. Also, the synthetic efficiency of the methodology was demonstrated by a gram scale experiment and by further converting them into 3‐nitro‐α‐carbolines.
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