Triethylamine → N-{4-[(6,7-Dimethoxy-4-quinolyl)oxy]-3-fluorophenyl}-N'-[1-(5-methyl-1,3-thiazol-2-yl)ethyl]urea

HRID 1817481ノート

反応式

HRID 1817481 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])=[CH:18][C:17]=1[F:23].C(N(CC)CC)C.ClC(Cl)(O[C:35](=[O:41])OC(Cl)(Cl)Cl)Cl.[CH3:43][C:44]1[S:48][C:47]([CH:49]([NH2:51])[CH3:50])=[N:46][CH:45]=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:35]([NH:51][CH:49]([C:47]2[S:48][C:44]([CH3:43])=[CH:45][N:46]=2)[CH3:50])=[O:41])=[CH:18][C:17]=1[F:23]

参加物

6

反応物 4

HCID 8471TriethylamineHCID 94429TriphosgeneHCID 114269974-((6,7-Dimethoxyquinolin-4-yl)oxy)-3-fluorobenzenamineHCID 242744731-(5-Methyl-1,3-thiazol-2-yl)ethan-1-amine

生成物 1

HCID 10050926N-{4-[(6,7-Dimethoxy-4-quinolyl)oxy]-3-fluorophenyl}-N'-[1-(5-methyl-1,3-thiazol-2-yl)ethyl]urea収率 35%

試薬・触媒・溶媒 1

HCID 6212Chloroform溶媒3 回

実験手順

4-[(6,7-Dimethoxy-4-quinolyl)oxy]-3-fluoroaniline (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-(5-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 (16 mg, yield 35%).

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-f250a00007be4dbe8e33e4d76b21f379
出典データセット
uspto-grants-2009_10
特許番号
US07598258B2

反応ノート

読み込み中…