反应详情

D,L-Serine methyl ester hydrochloride (2.1 mmol) and 5-chloro-1H-indole-2-carboxylic acid (2.0 mmol) were coupled according to Procedure A (0-25° C. reaction temperature, washed with acid first then with saturated NaHCO3) and the product purified by chromatography on silica gel eluted with 10, 20, 40 and 60% ethyl acetate in hexanes: Yield 565 mg, 95%; HPLC (60/40) 3.46 minutes (98%); mp 153-155 ° C.; TSPMS 297/299 (MH+, 100/40%);

1. custom0-25° C. reaction temperature
2. washwashed with acid first
3. customwith saturated NaHCO3) and the product purified by chromatography on silica gel
4. washeluted with 10, 20, 40 and 60% ethyl acetate in hexanes
5. customHPLC (60/40) 3.46 minutes (98%)