[C:1]([O:4][CH2:5][C:6]1[C:7]([N:31]2[CH2:42][CH2:41][N:40]3[C:33](=[CH:34][C:35]4[CH2:36][C:37]([CH3:44])([CH3:43])[CH2:38][C:39]=43)[C:32]2=[O:45])=[N:8][CH:9]=[CH:10][C:11]=1[C:12]1[CH:17]=[C:16]([NH:18][C:19]2[CH:24]=[CH:23][CH:22]=[C:21]([O:25][CH2:26][CH2:27][NH2:28])[N:20]=2)[C:15](=[O:29])[N:14]([CH3:30])[CH:13]=1)(=[O:3])[CH3:2].[C:46](Cl)(=[O:49])[CH:47]=[CH2:48]>C(Cl)Cl>[C:1]([O:4][CH2:5][C:6]1[C:7]([N:31]2[CH2:42][CH2:41][N:40]3[C:33](=[CH:34][C:35]4[CH2:36][C:37]([CH3:44])([CH3:43])[CH2:38][C:39]=43)[C:32]2=[O:45])=[N:8][CH:9]=[CH:10][C:11]=1[C:12]1[CH:17]=[C:16]([NH:18][C:19]2[CH:24]=[CH:23][CH:22]=[C:21]([O:25][CH2:26][CH2:27][NH:28][C:46](=[O:49])[CH:47]=[CH2:48])[N:20]=2)[C:15](=[O:29])[N:14]([CH3:30])[CH:13]=1)(=[O:3])[CH3:2]To a solution of 101e (250 mg, 0.387 mmol) and TEA (78 mg, 0.77 mmol) in DCM (10 mL) was added dropwise a solution of acryloyl chloride (42 mg, 0.46 mmol) in DCM. This mixture was stirred at room temperature for 2 h. The mixture was concentrated under reduce pressure to afford 101f as a yellow solid (crude), which was used in next step without further purification. MS-ESI: [M+H]+ 666.4
Wird geladen…