A facile, one‐step, direct functionalization of the C1 and N positions of tetrahydroisoquinolines was developed. Unprotected tetrahydroisoquinolines, indoles, and benzaldehydes could be used as starting materials. The different substituted indoles and benzaldehydes were investigated in detail and the scope proved to be broad.
Unsubstituted tetrahydroisoquinoline (I) is treated with various benzaldehydes or cyclohexanealdehyde and indoles under conditions A) which include an optimized catalytic system consisting of 3 components.
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