反应详情

2,5-dioxopyrrolidin-1-yl 3-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanoate (0.65 g, 2.43 mmol) was added to a solution of crude N-(3-(4-(4-((3-(2-(2-(3-aminopropoxy)ethoxy)ethoxy)propyl)amino)-benzoyl)phenoxy)propyl)-1-(5-(2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamido)-3,6,9,12-tetraoxapentadecan-15-amide (2 g, 2.11 mmol) in DCM (20 mL) and the reaction mixture was stirred for 2 hs at room temperature. Upon completion, reaction was then concentrated under reduced pressure, and purified by silica gel chromatography (DCM to DCM:MeOH, gradient) to yield 1.70 g (1.55 mmol, 73%) N-(3-(4-(4-((17-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-15-oxo-4,7,10-trioxa-14-azaheptadecyl)-amino)benzoyl)phenoxy)propyl)-1-(5-(2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamido)-3,6,9,12-tetraoxapentadecan-15-amide as yellow oil.

1. customUpon completion, reaction
2. concentrationwas then concentrated under reduced pressure
3. custompurified by silica gel chromatography (DCM to DCM:MeOH, gradient)