1,3-Dibromo-5,5-dimethylhydantoin → 5-Bromo-7-(3-methoxyphenyl)-6-(3-(pyrrolidin-1-yl)propyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine
反応式
[CH3:1][O:2][C:3]1[CH:4]=[C:5]([C:9]2[N:17]3[C:12]([C:13]([NH2:18])=[N:14][CH:15]=[N:16]3)=[CH:11][C:10]=2[CH2:19][CH2:20][CH2:21][N:22]2[CH2:26][CH2:25][CH2:24][CH2:23]2)[CH:6]=[CH:7][CH:8]=1.[Br:27]N1C(C)(C)C(=O)N(Br)C1=O>CN(C=O)C>[Br:27][C:11]1[C:10]([CH2:19][CH2:20][CH2:21][N:22]2[CH2:26][CH2:25][CH2:24][CH2:23]2)=[C:9]([C:5]2[CH:6]=[CH:7][CH:8]=[C:3]([O:2][CH3:1])[CH:4]=2)[N:17]2[C:12]=1[C:13]([NH2:18])=[N:14][CH:15]=[N:16]2参加物
4
反応物 2
生成物 1
試薬・触媒・溶媒 1
実験手順
To a solution of the compound (98 mg, 0.28 mmol) prepared in Example 14 in DMF (4 mL) at −40° C. was added 1,3-dibromo-5,5-dimethylimidazolidine-2,4-dione (40 mg, 0.14 mmol) portion wise over a period of 1 minute. The reaction was stirred for 30 minutes and was allowed to warm to room temperature, and stirred overnight. DMF was removed, and the crude solid was extracted with sodium hydroxide (1N) and DCM. The organic layer was dried, concentrated to obtain the title compound (97 mg) having the following physical data.