Heterocycles p. 2581 - 2592 (2010)
Update date:2022-09-26
Topics:
Cheng, Jianjun
Fu, Liqiang
Ling, Chenyu
Yang, Yushe
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. The Japan Institute of Heterocyclic Chemistry.
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