反应详情

To a solution of the compound of Example 48 (50 mg, 127 μmol) in THF (2 mL) and DMF (2 mL), EDC hydrochloride (27 mg, 139 μmol), HOBt (19 mg, 139 μmol), DIPEA (25 mg, 190 μmol) and BOC-sarcosine (26 mg, 139 μmol) is added. The mixture is stirred at rt for 1 h before it is concentrated. The residue is dissolved in 4 M HCl in dioxane (2 mL) and the mixture is stirred at rt for 30 min, concentrated and separated by prep. HPLC to give the title compound (23 mg) as a reddish oil; LC-MS: tR=0.89 min, [M+H]+=466.05.

1. concentrationis concentrated
2. dissolutionThe residue is dissolved in 4 M HCl in dioxane (2 mL)
3. stirringthe mixture is stirred at rt for 30 min
4. concentrationconcentrated
5. customseparated by prep