反应详情

Combine 2-isopropyl-5H-dibenzo[b,e][1,4]diazepin-11-ylamine (0.665 g, 2.31 mmol) and (S)-2-[2-(3-fluoro-phenyl)-ethyl]-piperazine (0.962 g, 4.62 mmol)in toluene (4.0 mL) and DMSO (1.0 mL) and heat at 110° C. for 18 hours. Cool to ambient temperature and dilute with ethyl acetate (75 mL). Wash with 0.1N NaOH solution, water and evaporate to give 0.996 g of the crude product. Silica gel chromatography, eluting with methylene chloride: 2N NH3/methanol (100:4), gives 0.216 g of the title compound as a tan solid: mass spectrum (ion spray): n/z=443 (M+1).

1. washWash with 0.1N NaOH solution, water
2. customevaporate
3. customto give 0.996 g of the crude product
4. washSilica gel chromatography, eluting with methylene chloride