Manufacturing Process
A mixture of 4.1 parts of N-[4-(methoxymethyl)-4-piperidinyl]-Nphenylpropanamide,
5.3 parts of sodium carbonate and 120 parts of 4-
methyl-2-pentanone is stirred and refluxed with water-separator. Then there
are added 4.1 parts of 2-thiopheneethanol methanesulfonate ester and stirring
at reflux is continued for 18 hours. The reaction mixture is cooled, washed
twice with water and evaporated. The oily residue is purified by columnchromatography
over silica gel, using a mixture of trichloromethane and 5%
of methanol as eluent. The first fraction is collected and the eluent is
evaporated. The oily residue is converted into the hydrochloride salt in 2,2'-
oxybispropane. The free base is liberated again in the conventional manner.
After extraction with 2,2'-oxybispropane, the latter is dried, filtered and
evaporated. The oily residue solidifies on triturating in petroleum-ether. The
solid product is filtered off and crystallized from petroleum-ether at -20°C,
yielding, after drying, N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-
piperidinyl]-N-phenylpropanamide; melting point 98.6°C.
