反应详情

2-Amino-3-((1-(3-(imidazol-2-ylamino)propyl)(1H-indazol-5-yl))carbonylamino)propanoic acid (0.050 g, 0.103 mmol) was dissolved in N,N-dimethylformamide (2 mL). Triethylamine (43.1 μL, 0.309 mmol) was added and the reaction was stirred for 5 minutes. A precipitate formed so methyl sulfoxide (1 mL) was added. Succinimidyl N-boc-6-aminohexanoate (0.0406 g, 0.124 mmol) was added and the reaction was stirred under N2 for 18 h. The reaction was then concentrated to an oil under high vacuum. The oil was purified by the following method (Preparative HPLC Method A) to give 39.9 mgs (66%) of product. ESMS: Calcd. for C28H40N8O6, 584.31. Found, 585.2 [M+H]+1. Analytical HPLC, Method B, Rt=18.72 min, Purity=98% Preparative HPLC Method A:

1. additionwas added
2. stirringthe reaction was stirred under N2 for 18 h
3. concentrationThe reaction was then concentrated to an oil under high vacuum
4. customThe oil was purified by the following method (Preparative HPLC Method A)