Abstract–A new synthetic strategy of (S)-(−)-stepholidine, a promising antipsychotic drug candidate, is described. Nucleophilic addition of a laterally lithiated nitrile to a (S)-tert- butanesulfinylimine was used as the key step, which was complished in 94% de and the main isomer was isolated in 52% yield.(S)-(−)-Stepholidine was prepared after another 5 steps, with an overall yield of 18.3% and> 98% ee.
