반응 #2446076
ord-0ba85b18f15447e783acc542db195919
반응 방정식
3-aminopropan-1-ol
Auristatin F
HATU
diisopropylethylamine
→
title compound
수율 68.0%
Auristatin F hydroxypropylamide
수율 68.0%
용매
반응 조건
온도
23°CELSIUS
상세 조건
See reaction.notes.procedure_details.
후처리
- 1기타Reduction of the volume to 1.4 mL under high vacuum followed by purification via preparative HPLC (10-90 solvent B gradient over 20 minutes eluting with 0.1% TFA/Water, 0.1% TFA/CH3CN)
실험 절차
Auristatin F (150 mg, 0.201 mmol), HATU (153.0 mg, 0.402 mmol), and diisopropylethylamine (108 μL, 0.603 mmol) were taken up in DMF (5 mL) and 3-aminopropan-1-ol (45.9 μL, 0.603 mmol) was added. The mixture was stirred at 23° C. for 45 minutes at which time LCMS analysis showed complete disappearance of the starting material. Reduction of the volume to 1.4 mL under high vacuum followed by purification via preparative HPLC (10-90 solvent B gradient over 20 minutes eluting with 0.1% TFA/Water, 0.1% TFA/CH3CN) afforded the title compound as white solid (109 mg, 68% yield).