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Edraw Max 7.2 Crack Free Download.The present invention relates to a process for the production of 1-cyclohexyl-4-(2,2,2-trifluoroethyl)piperidine, a useful medicament and a synthetic intermediate.
It has been found that 1-cyclohexyl-4-(2,2,2-trifluoroethyl)piperidine is a useful medicament. The process for the preparation of this compound is the subject matter of the present invention.
N,N-di(2,2,2-trifluoroethyl)piperidino is a synthetic intermediate in the preparation of the medicament, which is the subject matter of another patent application by the present applicant.
According to the present invention, 1-cyclohexyl-4-(2,2,2-trifluoroethyl)piperidine is prepared by reacting cyclohexyl isocyanide with 1-(2,2,2-trifluoroethyl)-4-(2,2,2-trifluoroethyl)piperidine. 1-(2,2,2-Trifluoroethyl)piperidine is reacted according to process known from the prior art with acrylonitrile in the presence of water and by addition of organic solvents. The reaction is carried out in the presence of reaction catalyst. The reaction preferably takes place in an inert solvent, e.g. in tetrahydrofuran or methylene chloride in the presence of a strong base, e.g. K2CO3 or Na2CO3. Addition of 1,2-dichloroethane, oleyl chloride and toluene can increase the yield in the reaction.
The alkyl isocyanide is preferably cyclohexyl isocyanide. The ester of 1-(2,2,2-trifluoroethyl)-4-(2,2,2-trifluoroethyl)piperidine is preferably a saturated ester of 1-(2,2,2-trifluoroethyl)-4-(2,2,2-trifluoroethyl)piperidine. The reaction is preferably carried out at temperature from xe2x88x9210 to 40xc2x0 C.
The 1-(2,2,2-trif
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