Benzphetamine hydrochloride

42 parts of para-butylamino-benzoic acid ethyl ester are put with 16.0 parts of a mixture of polyethylene glycol monomethyl ethers, boiling at 1B0°-220°C at a pressure of 0.01 mm of mercury, in a closed reaction vessel which Is fitted with an adjustable inlet tube for solvents and a connection for distilling off in vacuo. In order to dry the mixture completely, it is heated for an hour at 100°-105°C and absolute xylene is introduced under the surface of the mixture in vacuo at a pressure of 12 mm of mercury. There is thus a constant stream of xylene steam passing through the whole apparatus, which removes the last traces of moisture and any other volatile impurities. The xylene is condensed in a cooler. The whole is cooled to 20°-30°C and 0.06 part of sodium methylate dissolved in 0.6 part of methanol is added. 

Thereupon xylene is introduced again in vacuo at a temperature of 100°-105°C whereby all the methanol and the ethanol formed during re-esterification evaporates. The re-esterif-ication is continued under these conditions until a specimen of the reaction mass is clearly soluble in cold water, which occurs after about 2-3 hours. There is now obtained in almost quantitative yield the ester of the formula 

Chemical Name N-o -dimethyl-N-lphenylmethyDbenzeneethanamine hydrochloride Common Name — 

The benzene was distilled from the extract and the residue of d-N-methyl-N-benzyl-)3-phenyl-isopropylamine was distilled at reduced pressure. The thus obtained free base, distilling at 127°C at a pressure of 0.2 mm of mercury and having an np of 1.5515, was dissolved in ethyl acetate and a molar equivalent of ethanolic hydrogen chloride was added thereto. Anhydrous ether was added to the mixture and d-N-methyl-N-benzyl-)3-phenylisopropyl-amine hydrochloride precipitated from the reaction mixture as an oil which was crystallized from ethyl acetate to give crystals melting at 129° to 130°C. 

Matter, M. U.S. Patent 2,714,608 August 2, 1955 assigned to Ciba Pharmaceutical Products, Inc. 

Chemical Name N-a-dimethyl-N-(phenylmethyl)benzeneethanamine hydrochloride Common Name — 

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BENZPHETAMINE HYDROCHLORIDE Initiate dosage with 25 to 50 mg once/day increase according to response. Dosage ranges from 25 to 50 mg, 1 to 3 times/day. DIETHYLPROPION HYDROCHLORIDE ... 

Pregnancy (Category X - benzphetamine hydrochloride Category C - sibutramine, phentermine, phendimetrazine Category B - diethylpropion). 

Benzphetamine hydrochloride is an anorexiant that stimulates the satiety center in the brain, causing appetite suppression. It is used in 25 to 50 mg p.o. daily as a short-term (few weeks) adjunct to diet plan to reduce weight (see Amphetamine Sulfate). 

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