反应详情

4-(3-Aminopropyl)morpholine (0.34 mmol) and 2-[(5-chloro-1H-indole-2-carbonyl)-amino]-3-phenyl-propionic acid (0.30 mmol) were coupled according to Procedure A (0-25° C. reaction temperature) substituting the following workup: the reaction was diluted with ethyl acetate, the resulting solution washed three times with 2N NaOH and once with brine, dried over Na2SO4, and concentrated. The residue was stirred under ether for 1 hour, the solid filtered and dried: Yield 125 mg, 87%; HPLC (60/40) 2.85 minutes (98%); PBMS 469/471 (MH+, 100/90%);

1. washthe resulting solution washed three times with 2N NaOH
2. dry with materialonce with brine, dried over Na2SO4
3. concentrationconcentrated
4. filtrationthe solid filtered
5. customdried
6. customHPLC (60/40) 2.85 minutes (98%)