反应详情

(S)-2-Amino-3-phenyl-1-thiazolidin-3-yl-propan-1-one hydrochloride (4.0 mmol) and 5-cyano-1H-indole-2-carboxylic acid (4.0 mmol) were coupled according to Procedure A (0-25° C. reaction temperature, 48 hours reaction time) with the following workup: the reaction mixture was diluted with ethyl acetate and 2 N HCl, the resulting precipitate collected by filtration, washed with 2 N HCl and 2 N NaOH. The crude product was purified by chromatography on silica gel eluted with 30, 40 and 60% ethyl acetate in hexanes. Yield 1.22 g, 75%; HPLC (60/40) 4.74 minutes (97%); PBMS 405 (MH+, 100%);

1. filtrationthe resulting precipitate collected by filtration
2. washwashed with 2 N HCl and 2 N NaOH
3. customThe crude product was purified by chromatography on silica gel
4. washeluted with 30, 40 and 60% ethyl acetate in hexanes
5. customHPLC (60/40) 4.74 minutes (97%)