859964-70-8

Upstream product

• 1448-52-8 N,N-bis(2-chloroethyl)-4-methoxybenzenamine 
• 140-29-4 phenylacetonitrile 
• 104-94-9 4-methoxy-aniline 
• 19721-54-1 2-[(2-hydroxyethyl)-(4-methoxyphenyl)amino]ethanol 

Downstream Products

• 859964-86-6 1-(4-hydroxy-phenyl)-4-phenyl-piperidine-4-carboxylic acid 

Relevant academic research and scientific papers

A 4-substituted piperidine derivatives synthetic method

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.

A convenient one-pot preparation of N-substituted 4-phenylpiperidines

N-Substituted 4-phenylpiperidines were readily synthesized by one-pot cyclization of diols with amines via bis-triflate intermediates. The new synthesis under mild conditions gave various N-substituted 4-phenylpiperidines in moderate to good yields.