Abstract
AbstractAn efficient and versatile method for the synthesis of indole‐based polycyclic indolo‐benzazepine and its derivatives through water‐accelerated cationic π‐cyclisation is described. The strategy involves condensation of arylamine moieties linked to C‐4 in indole/azaindole systems with arylaldehydes in water containing catalytic amount of Brønsted acids. The C–C bond formation in water is complete within 10–30 min, furnishing the title compounds in excellent yields and purities, whereas in organic solvents 10–12 h are required. Furthermore, aldehydes both with electron‐donating and‐withdrawing substituents facilitate the π‐cyclisation equally.
Published Version
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