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摘要
This paper describes a rapid and practical synthetic route involving six-step reactions towards the diastereoselectively synthesis of (+/-)-endo-Epibatidine, starting from 6-chloro-3-pyridinecarboxaldehye. The effective Henry reaction gave precursor (E)-6-(6-chloropyridin-3-yl)-5-nitrohex-5-en-2-one (3a) which could be used in the next step. Various benzoic acid derivatives were used to optimize intramolecular Michael addition of ketone to pyridinylnitroolefins to provide the key intermediate 3-(6-chloropyridin-3-yl)-4-nitrocyclohexanone ((+/-)-7a) with high yield.
- 出版日期2012-6
- 单位华东理工大学
