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PROCESS FOR THE SYNTHESIS OF HIGHLY FUNCTIONALIZED RACEMIC AND NON-RACEMIC PIPERIDINES
PROCESS FOR THE SYNTHESIS OF HIGHLY FUNCTIONALIZED RACEMIC AND NON-RACEMIC PIPERIDINES
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机译：高度功能化的非无规哌啶类化合物的合成方法
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摘要
The present invention relates to a process for the synthesis of highly functionalized 2,6-disubstituted piperidines with syn-stereoselectivity via a domino intermolecular imino aldol follewd by an intramolecular aza-Michael reaction sequence in good yield. The process involves i) the synthesis of α-arylmethylidine- and α-alkylmethylidine-ß-keto ester as the precursor substrates, ii) generation of the enolate with LDA followed by reaction with N-sulfonyl aldimines.
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