反应详情

Acetic acid 2-[4-(4-cyano-2-methanesulfonyl-phenyl)-2,5-dioxo-1-(3-trifluoromethyl-phenyl)-1,4,5,6,7,8-hexahydro-2H-quinazolin-3-yl]-ethyl ester (step 1, 60.0 mg, 0.10 mmol) is stirred with trifluoroacetic acid (3.0 mL, 36.94 mmol) at 60° C. for 6 h and concentrated under reduced pressure. The residue is stirred over night with acetonitrile and water (→hydrolysis of trifluoroacetic acid ester) and then purified by reversed phase HPLC (Waters SunFire™-C18, gradient of acetonitrile in water, 0.1% TFA). Yield: 31.3 mg; ESI mass spectrum [M+H]+=534; Retention time HPLC: 0.78 min (005_CA01).

1. concentrationconcentrated under reduced pressure
2. custompurified by reversed phase HPLC (Waters SunFire™-C18, gradient of acetonitrile in water, 0.1% TFA)
3. custom0.78 min (005_CA01)