Abstract
An efficient and protecting‐group‐directed highly diastereoselective (≥ 99:1) synthesis of tetrahydro‐3H‐pyrrolo[2,3‐c]quinolines bearing four contiguous chiral centers was achieved by using intermolecular Michael addition followed by intramolecular Mannich cyclization strategy. The domino reaction proceeded well with a broad scope of substrates under mild conditions and afforded the corresponding products in good to excellent yields. The synthetic protocol provided a straightforward synthetic route to tetrahydropyrroloquinolines as single diastereomers, which are difficult to synthesize by other methodologies.
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