Hydrochloric Acid → Atomoxetine Hydrochloride
反応式
[ClH:1].[CH3:2][C:3]1[CH:4]=[CH:5][CH:6]=[CH:7][C:8]=1[O:9][C@@H:10]([C:15]1[CH:16]=[CH:17][CH:18]=[CH:19][CH:20]=1)[CH2:11][CH2:12][NH:13][CH3:14]>C(OCCCC)(=O)C>[ClH:1].[CH3:14][NH:13][CH2:12][CH2:11][C@@H:10]([O:9][C:8]1[CH:7]=[CH:6][CH:5]=[CH:4][C:3]=1[CH3:2])[C:15]1[CH:16]=[CH:17][CH:18]=[CH:19][CH:20]=1参加物
4
実験手順
Under stirring and maintaining temperature between 22° C. and 25° C. by means of water bath cooling, 10.07 g (0.09945 mol) of aqueous hydrogen chloride (36%) were dropped on 177 g (0.08648 mol) of atomoxetine base solution (n-butyl acetate), prepared as in Example 7. The hydrochloride then crystallized. The obtained suspension was stirred at about 25° C. for one hour. The solid was collected by filtration and washed twice with 30 ml of n-butyl acetate each time. The solid collected was dried for 18 hours at 70° C. under vacuum. Tomoxetine hydrochloride content: >99% by HPLC assay. Weight: 25.18 g (0.08629 mol). Yield: 99.8%. Atomoxetine hydrochloride enantiomeric ratio: R/S>99/1 (by chiral HPLC)