An approach to 1-alkyl-3-phenylpiperidine derivatives containing 2,5-functionalized groups: 1-methyl-2-(4-chlorophenylthiomethyl)-5-(methoxycarbonyl)- piperidine.
作者:Heleni K. Kotzamani、Christos G. Gourdoupis、Ioannis K. Stamos
DOI:10.1016/s0040-4020(01)89587-9
日期:1994.1
initial attack of methylamine on the bromoacrylic ester to give the methyl α-(methylamino)methylacrylate. Reaction with ketone then leads to intermediate acrylicenamine formation followed by cyclization to the unsaturated piperidine ring. Reduction of this cyclic with sodiumcyanoborohydride in the presence of carboxylic acid produced the piperidine derivative 1-methyl-2-(4-chlorophenylthiomethyl)-
Disclosed are compounds of formula X,
which are useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions comprising compounds of formula X and methods of preparing the compounds of formula X are also disclosed.