科研之友
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摘要
Cyclocondensation between acyclic 5-aminopent-2-enoate esters and aliphatic aldehydes containing an unsubstituted alpha-methylene unit affords 1,2,3,4-tetrahydropyridine derivatives in good yields. The reaction has been applied to a range of aldehydes, showing good functional group tolerance. Chemoselective hydride reduction of the enamine double bond provides 3,4-disubstituted tertiary piperidine derivatives with acceptable to good diastereoselectivities, whereas catalytic hydrogenation of N-benzyl derivatives leads directly to the corresponding secondary piperidines.
- 出版日期2010-2
