反应详情

4-(3Aminopropyl)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 2 N 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 2 N 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%)