Diisopropylethylamine → 8-Fluoro-11-[3-(3-methoxy-propyl)-piperazin-1-yl]-2-trifluoromethyl-5h-dibenzo[b,e][1,4]diazepine

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Reaction Conditions

Reaction Steps

Combine 8-fluoro-2-trifluoromethyl-5H-dibenzo[b,e][1,4]diazepin-11-ylaminehydrochloride (0.201 g, 0.606 mmol), (S)-2-(3-methoxy-propyl)-piperazine (0.192 g, 1.21 mmol), and diisopropylethyl amine (0.106 mL, 0.606 mmol) in a mixture of toluene (3 mL) and dimethylsulfoxide (1 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 8-fluoro-11-[3-(3-methoxy-propyl)-piperazin-1-yl]-2-trifluoromethyl-5H-dibenzo[b,e][1,4]diazepine (0.151 g, 0.346 mmol, 57%) as a yellow oil. Mass spectrum (APCI): m/z=437.2 (M+1).

Provenance & Evidence