Triethylamine → N-{4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2-methoxyphenyl}-N'-[1-(4-methyl-1,3-thiazol-2-yl)ethyl]urea

HRID 1817469ノート

反応式

HRID 1817469 の反応式
[CH3:1][O:2][C:3]1[CH:4]=[C:5]2[C:10](=[CH:11][C:12]=1[O:13][CH3:14])[N:9]=[CH:8][CH:7]=[C:6]2[O:15][C:16]1[CH:22]=[CH:21][C:19]([NH2:20])=[C:18]([O:23][CH3:24])[CH:17]=1.C(N(CC)CC)C.ClC(Cl)(O[C:36](=[O:42])OC(Cl)(Cl)Cl)Cl.[CH3:44][C:45]1[N:46]=[C:47]([CH:50]([NH2:52])[CH3:51])[S:48][CH:49]=1>C(Cl)(Cl)Cl>[CH3:1][O:2][C:3]1[CH:4]=[C:5]2[C:10](=[CH:11][C:12]=1[O:13][CH3:14])[N:9]=[CH:8][CH:7]=[C:6]2[O:15][C:16]1[CH:22]=[CH:21][C:19]([NH:20][C:36]([NH:52][CH:50]([C:47]2[S:48][CH:49]=[C:45]([CH3:44])[N:46]=2)[CH3:51])=[O:42])=[C:18]([O:23][CH3:24])[CH:17]=1

参加物

6

反応物 4

HCID 8471TriethylamineHCID 94429TriphosgeneHCID 45587211-(4-Methyl-1,3-thiazol-2-yl)ethan-1-amineHCID 218910314-((6,7-Dimethoxyquinolin-4-yl)oxy)-2-methoxyaniline

生成物 1

HCID 10435845N-{4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2-methoxyphenyl}-N'-[1-(4-methyl-1,3-thiazol-2-yl)ethyl]urea収率 48.4%

試薬・触媒・溶媒 1

HCID 6212Chloroform溶媒3 回

実験手順

4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2-methoxyaniline (30 mg) was dissolved in chloroform (1 ml) and triethylamine (0.1 ml) to prepare a solution. A solution of triphosgene (35 mg) in chloroform (0.2 ml) was then added to the solution, and the mixture was stirred at room temperature for one hr. Next, a solution of 1-(4-methyl-1,3-thiazol-2-yl)-1-ethylamine (35 mg) in chloroform (0.2 ml) was added thereto, and the mixture was stirred at room temperature for 10 hr. The stirred mixture was purified by chromatography on silica gel using chloroform/methanol for development to give the title compound (22 mg, yield 48%).

後処理

  1. stirringthe mixture was stirred at room temperature for 10 hr
  2. customThe stirred mixture was purified by chromatography on silica gel

出典と根拠

ORDレコード
ord-44e3407a0b794dc6a33d387eb0ba790c
出典データセット
uspto-grants-2009_10
特許番号
US07598258B2

反応ノート

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