反应详情

Sorafenib derivative S-6: S-5 (180 mg; 0.30 mmol) was dissolved in acetonitrile (3 ml), and a solution of N,N,N′,N′-tetramethyl-O—(N-succimidyl)uronium tetrafluoroborate (TSTU) (99 mg; 0.32 mmol) in acetonitrile (3 ml) was added, and N,N-diisopropylethylamine (67 μl; 0.37 mmol) was added. HPLC shows complete reaction after 10 min. 0.1% TFA in water (2 ml) is added, and the mixture is purified preparatively HLPC. S-6 is obtained as “off-white” solid substance (163 mg; 0.24 mmol; 78%). MS: M+H=692.1368; calculated for C30H25ClF3N5O9: 692.1371.

1. customreaction after 10 min
2. customthe mixture is purified preparatively HLPC
3. customS-6 is obtained as “off-white” solid substance (163 mg; 0.24 mmol; 78%)