反应详情

温度

100 °C

A stirred suspension of 2,6-dichloro-N-(cyclohexylmethyl)quinoline-5-carboxamide (Example 43(a)) (200 mg) and (3R)-3-pyrrolidinamine (0.20 mL) in acetonitrile (2 mL) was heated at 100° C. in a microwave for 1 hour after which it was cooled to room temperature and concentrated. The residue was purified by chromatography (SiO2, dichloromethane:methanol:ammonia in methanol (7 M) (95:5:1), and then by HPLC (Symmetry—0.1% aqueous trifluoroacetic acid/acetonitrile). Conversion to the dihydrochloride salt by treatment with hydrochloric acid (4M in 1,4-dioxane) and subsequent recrystallisation (methanol/ethyl acetate) afforded the title compound as a solid (46 mg).

1. temperaturewas cooled to room temperature
2. concentrationconcentrated
3. customThe residue was purified by chromatography (SiO2, dichloromethane
4. customConversion to the dihydrochloride salt by treatment with hydrochloric acid (4M in 1,4-dioxane) and subsequent recrystallisation (methanol/ethyl acetate)