Diisopropylethylamine → HCID 178493855、化合物

HRID 1259504

反応式

HRID 1259504 の反応式
[CH3:1][O:2][C:3]1[C:12]2[N:11]=[C:10]([NH2:13])[N:9]3[CH2:14][CH2:15][N:16]=[C:8]3[C:7]=2[CH:6]=[CH:5][C:4]=1[O:17][CH2:18][CH2:19][CH2:20][N:21]1[CH2:26][CH2:25][O:24][CH2:23][CH2:22]1.[NH2:27][C:28]1[CH:33]=[C:32]([C:34](O)=[O:35])[CH:31]=[CH:30][N:29]=1.C1CN([P+](ON2N=NC3C=CC=CC2=3)(N2CCCC2)N2CCCC2)CC1.F[P-](F)(F)(F)(F)F.C(N(C(C)C)CC)(C)C>CN(C=O)C>[NH2:27][C:28]1[CH:33]=[C:32]([CH:31]=[CH:30][N:29]=1)[C:34]([NH:13][C:10]1[N:9]2[CH2:14][CH2:15][N:16]=[C:8]2[C:7]2[CH:6]=[CH:5][C:4]([O:17][CH2:18][CH2:19][CH2:20][N:21]3[CH2:22][CH2:23][O:24][CH2:25][CH2:26]3)=[C:3]([O:2][CH3:1])[C:12]=2[N:11]=1)=[O:35]

参加物

6

反応物 4

HCID 81531DiisopropylethylamineHCID 2783962-Aminopyridine-4-carboxylic acidHCID 2724699PyBOPHCID 178493860HCID 178493860、化合物

生成物 1

HCID 178493855HCID 178493855、化合物収率 37.2%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

7-Methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-amine (100 mg, 0.28 mol) was dissolved in DMF (3 mL), and 2-aminopyridine-4-carboxylic acid (38 mg, 0.28 mmol) was added. PYBOP (217 mg, 0.42 mmol) and diisopropylethylamine (0.15 mL, 0.83 mmol) were subsequently added, and the mixture was stirred at rt overnight. The mixture was purified by HPLC to give the title compound (50 mg, 37%). LC MS RT=1.02 min, MH+=480.3. 1H NMR (DMSO-d6) δ: 13.25 (1H, br s), 10.15 (1H, br s), 8.42 (1H, br s), 8.08 (1H, s), 8.06 (1H, d), 7.43 (1H, d), 7.75 (1H, s), 7.50 (1H, d), 7.38 (1H, dd), 4.50 (2H, dd), 4.35 (2H, br t), 4.27 (2H, dd), 4.01 (3H, s), 3.99 (2H, br s), 3.66 (2H, t), 3.50 (2H, d), 3.31 (2H, br t), 3.13 (2H, m), 2.25 (2H, m).

後処理

  1. customThe mixture was purified by HPLC

出典と根拠

ORDレコード
ord-1b09de3ca90845aeb5718273284f3179
出典データセット
uspto-grants-2013_06
特許番号
US08466283B2

関連ノート

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