Diethyl Pyrocarbonate → HCID 68453853、化合物

反応式

[NH2:1][CH2:2][C:3]1[CH:8]=[C:7]([CH:9]=[CH2:10])[C:6]([NH:11][S:12]([CH3:15])(=[O:14])=[O:13])=[C:5]([F:16])[CH:4]=1.[C:17]([C:21]1[CH:26]=[CH:25][C:24]([CH:27]=[C:28]([CH3:32])[C:29](O)=[O:30])=[CH:23][CH:22]=1)([CH3:20])([CH3:19])[CH3:18].CCOC(OC(OCC)=O)=O>CN(C=O)C>[C:17]([C:21]1[CH:22]=[CH:23][C:24]([CH:27]=[C:28]([CH3:32])[C:29]([NH:1][CH2:2][C:3]2[CH:8]=[C:7]([CH:9]=[CH2:10])[C:6]([NH:11][S:12]([CH3:15])(=[O:14])=[O:13])=[C:5]([F:16])[CH:4]=2)=[O:30])=[CH:25][CH:26]=1)([CH3:20])([CH3:18])[CH3:19]

参加物

実験手順

N-(4-Aminomethyl-2-fluoro-6-vinylphenyl)methanesulfonamide (0.15 mmol, 54.21 mg), 3-(4-tert-butyl-phenyl)-2-methylacrylic acid (0.14 mmol, 30 mg), DEPC (1.2 eq, 0.17 mmol, 25.49 μl), and TEA (2 eq, 0.28 mmol, 39.03 μl) were added in DMF. The reaction mixture was stirred for 12 hrs. The reaction mixture was purified according to similar procedure of Example 21 to yield title product (34.8 mg, 55.96%).