反应详情

(S)-2-Amino-3-(4-fluoro-phenyl)-1-morpholin-4-yl-propan-1-one hydrochloride (0.48 mmol) and 5-fluoro-1H-indole-2-carboxylic acid (0.48 mmol) were coupled according to Procedure A (0-25° C. reaction temperature, 48 hour reaction time, washed with acid first then base) and the product purified by chromatography on silica gel eluted with 20, 30, 40, 50 and 75% ethyl acetate in hexanes. Yield 189 mg, 95%; HPLC (60/40) 4.76 minutes (97%); PBMS 414 (MH+, 100%);

1. custom0-25° C. reaction temperature, 48 hour reaction time
2. washwashed with acid first
3. custombase) and the product purified by chromatography on silica gel
4. washeluted with 20, 30, 40, 50 and 75% ethyl acetate in hexanes
5. customHPLC (60/40) 4.76 minutes (97%)