BigPatents India

The present invention relates to a process for preparing nitro-substituted, enantiomerically enriched 1-phenylethylamines, and to their use. 240.0 g (1.453 mol) of 3-nitroacetophenone are suspended at room temperature in 1200 ml of ethanol. A solution of 132.0 g of O-methyldroxylamine hydrochloride in 120 ml of water is added dropwise in 45 min to the suspension. The reaction mixture is heated to boiling and stirred at this temperature for 4th. The suspension is subsequently hot-filtered. The filtrate is cooled to room temperature over a period of 12h. The colourless soild which precipitaes out in this time is filtered off with suction using a frit and washed three times with 100 ml of ethanol each tin\me. The product is dried at 500C and a pressure of 100 mbar a period of 2h. 235.3 g (83.2% of theory) of a pale yellow solid are obtained.