反应详情

Following Scheme I, 18.1 parts of 4-diphenylmethylpiperidine (U.S. Pat. No. 3,806,526) 13.6 parts of 2-chloroethylpiperidine hydrochloride and 16 parts of sodium carbonate are placed in 250 parts of aqueous 95% ethanol and heated at reflux for 5 hours with stirring. The ethanol is removed to provide an oil which is 1-(2-piperidinoethyl)-4-(diphenylmethyl)piperidine. This oil is dissolved in anhydrous ethanol and 2 equivalents of hydrochloric acid gas are added to provide 1-(2-piperidinoethyl)-4-(diphenylmethyl)piperidine dihydrochloride, melting at 330° C. The anhydrous ethanol solution of 1-(2-piperidinoethyl)-4-(diphenylmethyl)piperidine is reacted with 1.5 equivalents of oxalic acid to provide the oxalic acid salt. In a similar manner other previously mentioned pharmaceutically acceptable salts are formed.

1. temperatureheated
2. temperatureat reflux for 5 hours
3. customThe ethanol is removed
4. customto provide an oil which