反应详情

Using 3-bromo-4-fluorobenzotrifluoride and following the procedures described in EXAMPLE 17, Parts B and C, (±)-cis tert-butyl 2-amino-4,5,7a,8,10,10a-hexahydrodipyrrolo[3,4-c:3′,2′,1′-ij]quinoline-9(7H)-carboxylate was converted into (±) -cis-N-[2-fluoro-5-(trifluoromethyl)phenyl]-4,5,7,7a,8,9,10,10a-octahydrodipyrrolo[3,4-c:3′,2′,1′-ij]quinolin-2-amine, bis-trifluoroacetic acid salt, after HPLC purification (C18 reverse phase column, elution with a H2O/CH3CN gradient with 0.5% TFA). This material was free-based with aq ammonium hydroxide, extracted with chloroform, washed with brine, dried (K2CO3) and concentrated to the title compound of EXAMPLE 115 as the free base. LRMS (ES)+: 378.3 (M+H)+.

1. customafter HPLC purification (C18
2. washphase column, elution with a H2O/CH3CN gradient with 0.5% TFA)
3. extractionextracted with chloroform
4. washwashed with brine
5. dry with materialdried (K2CO3)
6. concentrationconcentrated to the title compound of EXAMPLE 115 as the free base