Ammonia → 2-{4-[4-({4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-yl}amino)phenyl]piperazin-1-yl}-2-oxoethanol

HRID 1441309ノート

反応式

HRID 1441309 の反応式
C([O:4][CH2:5][C:6]([N:8]1[CH2:13][CH2:12][N:11]([C:14]2[CH:35]=[CH:34][C:17]([NH:18][C:19]3[N:24]=[C:23]([C:25]4[N:29]([CH:30]([CH3:32])[CH3:31])[C:28]([CH3:33])=[N:27][CH:26]=4)[CH:22]=[CH:21][N:20]=3)=[CH:16][CH:15]=2)[CH2:10][CH2:9]1)=[O:7])(=O)C.N>CO>[OH:4][CH2:5][C:6]([N:8]1[CH2:9][CH2:10][N:11]([C:14]2[CH:35]=[CH:34][C:17]([NH:18][C:19]3[N:24]=[C:23]([C:25]4[N:29]([CH:30]([CH3:32])[CH3:31])[C:28]([CH3:33])=[N:27][CH:26]=4)[CH:22]=[CH:21][N:20]=3)=[CH:16][CH:15]=2)[CH2:12][CH2:13]1)=[O:7]

参加物

4

反応物 2

HCID 222AmmoniaHCID 686898132-{4-[4-(2-Acetoxyacetyl)piperazin-1-yl]anilino}-4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)pyrimidine

生成物 1

HCID 112705002-{4-[4-({4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-yl}amino)phenyl]piperazin-1-yl}-2-oxoethanol

試薬・触媒・溶媒 1

HCID 887Methanol溶媒2 回

実験手順

2-{4-[4-(2-Acetoxyacetyl)piperazin-1-yl]anilino}-4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)pyrimidine (Example 21; 330 mg) was stirred in MeOH (5 ml) at room temperature and 7N ammonia in MeOH (1.6 ml) was added. After 28 hours, the reaction was evaporated under reduced pressure. Chromatography on silica gel using MeOH:DCM (4:96 to 5:95), yielded the title compound as a yellow solid. (108 mg 36%). NMR: 1.39 (d, 6H), 2.46 (s, 3H), 3.05 (b s, 4H), 3.48 (b s, 2H), 3.61 (b s, 2H), 4.12 (d, 2H), 4.57 (t, 1H), 5.69 (septuplet, 1H), 6.92 (d, 2H), 6.95 (d, 1H), 7.38 (s, 1H), 7.47 (d, 2H), 8.31 (d, 1H), 9.15 (s, 1H); m/z 436.

後処理

  1. customthe reaction was evaporated under reduced pressure

出典と根拠

ORDレコード
ord-7a3c34f467ef486aac1c149bd7c1d186
出典データセット
uspto-grants-2010_02
特許番号
US07655652B2

反応ノート

読み込み中…