Reaktion #738298

Reaktionsgleichung

(S)-2-Amino-3-(4-fluoro-phenyl)-1-morpholin-4-yl-propan-1-one hydrochloride

5-fluoro-1H-indole-2-carboxylic acid

→

5-Fluoro-1H-indole-2-carboxylic acid [(1S)-(4-fluoro-benzyl)-2-morpholin-4-yl-2-oxo-ethyl]-amide

Reaktionsbedingungen

Aufarbeitung

1. 1
   Sonstige0-25° C. reaction temperature, 48 hour reaction time
2. 2
   Waschenwashed with acid first
3. 3
   Sonstigebase) and the product purified by chromatography on silica gel
4. 4
   Wascheneluted with 20, 30, 40, 50 and 75% ethyl acetate in hexanes
5. 5
   SonstigeHPLC (60/40) 4.76 minutes (97%)

Vorschrift

(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%);

Quelle