反应详情

温度

110 °C

Combine 7-fluoro-2-trifluoromethyl-5H-dibenzo[b,e][1,4]diazepin-11-ylamine hydrochloride (0.399 g, 1.20 mmol), (S)-2-(3-methoxy-propyl)-piperazine (0.381 g, 2.41 mmol), and diisopropylethyl amine (0.21 mL, 1.20 mmol) in a mixture of toluene (4.5 mL) and dimethylsulfoxide (1.5 mL) and stir at 110° C. for 24 hours. Evaporate the mixture then purify by flash chromatography, eluting with a step gradient starting with dichloromethane going to 7% 2N ammonia-methanol in dichloromethane gives (s)-7-fluoro-11-[3-(3-methoxy-propyl)-piperazin-1-yl]-2-trifluoromethyl-5H-dibenzo[b,e][1,4]diazepine (0.268 g, 0.614 mmol, 51%) as a yellow oil. Mass spectrum (APCI): m/z=437.2 (M+1).

1. customEvaporate the mixture
2. customthen purify by flash chromatography
3. washeluting with a step gradient