2-Amino-4-chloro-6-methylpyrimidine → 2-Amino-4-[(4-{[(4-amino-2-methyl-6-quinolinyl)carbonyl]amino}benzyl)amino]-6-methylpyrimidine

HRID 19515

反応式

HRID 19515 の反応式
[NH2:1][C:2]1[C:11]2[C:6](=[CH:7][CH:8]=[C:9]([C:12]([NH:14][C:15]3[CH:22]=[CH:21][C:18]([CH2:19][NH2:20])=[CH:17][CH:16]=3)=[O:13])[CH:10]=2)[N:5]=[C:4]([CH3:23])[CH:3]=1.[NH2:24][C:25]1[N:30]=[C:29](Cl)[CH:28]=[C:27]([CH3:32])[N:26]=1.C(N(C(C)C)CC)(C)C>CN(C=O)C>[NH2:24][C:25]1[N:30]=[C:29]([NH:20][CH2:19][C:18]2[CH:21]=[CH:22][C:15]([NH:14][C:12]([C:9]3[CH:10]=[C:11]4[C:6](=[CH:7][CH:8]=3)[N:5]=[C:4]([CH3:23])[CH:3]=[C:2]4[NH2:1])=[O:13])=[CH:16][CH:17]=2)[CH:28]=[C:27]([CH3:32])[N:26]=1

参加物

5

反応物 3

HCID 218102-Amino-4-chloro-6-methylpyrimidineHCID 81531DiisopropylethylamineHCID 178646304-{[(4-Amino-2-methyl-6-quinolinyl)carbonyl]amino}benzylamine

生成物 1

HCID 103416612-Amino-4-[(4-{[(4-amino-2-methyl-6-quinolinyl)carbonyl]amino}benzyl)amino]-6-methylpyrimidine収率 82.2%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

The solution of 27 mg (0.05 mmol) 4-{[(4-amino-2-methyl-6-quinolinyl)carbonyl]amino}benzylamine, 15 mg (0.1 mmol) 2-amino-4-chloro-6-methylpyrimidine, and 0.05 ml (0.3 mmol) diisopropyl ethylamine in 1 ml DMF was stirred at 120° C. for 5 h. After evaporation of the solvent the residue was purified by HPLC and lyophilized to yield 17 mg (51%) of the title compound. MS 414.3 (M+1)+, 1H-NMR (DMSO-d6) δ 2.19 (s, 3H), 2.60 (s, 3H), 4.56 (d, 2H), 5.94 (s, 1H), 6.65 (s, 1H), 7.33 (d, 2H), 7.75 (d, 2H), 7.88 (d, 1H), 8.35 (d, 1H), 8.97 (s, 1H), 8.96-9.01 (m, 2H), 10.51 (s, 1H), 12.30 (br. 1H), 13.60 (br. 1H).

後処理

  1. customAfter evaporation of the solvent the residue
  2. customwas purified by HPLC

出典と根拠

ORDレコード
ord-30d280a04e5c4ef0b7b8413e0b5e46c6
出典データセット
uspto-grants-2010_06
特許番号
US07745443B2

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