Diisopropylethylamine → HCID 178493859、化合物

HRID 1259505ノート

反応式

HRID 1259505 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[S:29][C:30]([C:34](O)=[O:35])=[C:31]([CH3:33])[N:32]=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[S:29][C:30]([C:34]([NH:13][C:10]2[N:9]3[CH2:14][CH2:15][N:16]=[C:8]3[C:7]3[CH:6]=[CH:5][C:4]([O:17][CH2:18][CH2:19][CH2:20][N:21]4[CH2:22][CH2:23][O:24][CH2:25][CH2:26]4)=[C:3]([O:2][CH3:1])[C:12]=3[N:11]=2)=[O:35])=[C:31]([CH3:33])[N:32]=1

参加物

6

反応物 4

HCID 81531DiisopropylethylamineHCID 8322432-Amino-4-methyl-thiazole-5-carboxylic acidHCID 2724699PyBOPHCID 178493860HCID 178493860、化合物

生成物 1

HCID 178493859HCID 178493859、化合物収率 4.3%

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-amino-4-methylthiazole-5-carboxylic acid (44 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 (6 mg, 4%): LC MS RT=1.06 min, MH+=500.1; 1H NMR (DMSO-d6) δ: 12.59 (1H, s), 7.55 (1H, d), 7.47 (1H, s), 6.98 (1H, d), 4.13 (2H, t), 3.93 (4H, m), 3.86 (3H, s), 3.55 (4H, t), 2.47 (3H, s), 2.45 (2H, t), 2.33 (4H, m), 1.93 (2H, m).

後処理

  1. customThe mixture was purified by HPLC

出典と根拠

ORDレコード
ord-90a64149fe2645ca81c603f793b98cdf
出典データセット
uspto-grants-2013_06
特許番号
US08466283B2

反応ノート

読み込み中…