75354-98-2Relevant academic research and scientific papers
A 4-substituted piperidine derivatives synthetic method
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Paragraph 0073-0083, (2020/02/07)
The invention relates to a synthesis method of 4-substituted piperidine derivatives. The synthesis method comprises the following steps: continuously reacting alpha-single substituted acetonitrile serving as a raw material with two-molecular ethylene oxide in the presence of a base I, thereby synthesizing compounds (2), wherein not one compound (2) is generated, and the compounds (2) are in tautomeric equilibrium with a compound (6); breaking the balance in the presence of a base II to generate an alcoxyl negative ion compound (3); reacting the compound (3) with R2SO2X or (R2SO2)2O to generate sulphonates (4); performing a cyclization reaction on the sulphonates (4) and primary amine to synthesize 4-substituted piperidine derivatives. Compared with a document reported method, the synthesis method has the advantages that the reaction steps are shortened and the synthetic efficiency is improved.
