| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject compound useful as an appetite inhibitor in a high yield by reacting (phenylethyl)methyl(trifluoromethyl)benzeneethaneamine with an ethylating agent, subjecting the reaction product to a reductive debenzylation reaction and subsequently forming the salt of the reaction product. SOLUTION: This method for producing dexfenfluramine hydrochloride of formula III comprises reacting 1 mole (equivalent) of (S,S)-N-(1-phenylethyl)-α- methyl-3-(trifluoromethyl)benzeneethaneamine of formula I or its organic acid or inorganic acid salt with 1-3 moles of a quanternization-impossible tertiary amine in the presence of an alkali carbonate at 20-150 deg.C for 4-80 hr, hydrogenatively debenzylating the obtained compound of formula II in the presence of palladium-carbon as a catalyst in a hydrogenator in a polar solvent at 20-100 deg.C at 1-20 atm 1-8 hr, and subsequently forming the salt of the debenzylation product with hydrochloric acid.
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