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Diisopropylcarbodiimide → N-{4-Chloro-3-[5-chloro-1-methyl-6-(4-(4-trifluoromethylphenyl)piperazin-1-yl)-1H-benzimidazol-2-ylamino]-benzyl}-1-trifluoromethyl-cyclopropanamide

HRID 1258705
ノート
印刷プレビュー

反応式

HRID 1258705 の反応式
[Cl:1][C:2]1[CH:18]=[CH:17][C:5]([CH2:6][NH:7][C:8]([C:10]2([C:13]([F:16])([F:15])[F:14])[CH2:12][CH2:11]2)=[O:9])=[CH:4][C:3]=1[N:19]=[C:20]=S.[Cl:22][C:23]1[C:24]([N:32]2[CH2:37][CH2:36][N:35]([C:38]3[CH:43]=[CH:42][C:41]([C:44]([F:47])([F:46])[F:45])=[CH:40][CH:39]=3)[CH2:34][CH2:33]2)=[CH:25][C:26]([NH:30][CH3:31])=[C:27]([CH:29]=1)[NH2:28].CC(C)N=C=NC(C)C>>[Cl:1][C:2]1[CH:18]=[CH:17][C:5]([CH2:6][NH:7][C:8]([C:10]2([C:13]([F:16])([F:15])[F:14])[CH2:12][CH2:11]2)=[O:9])=[CH:4][C:3]=1[NH:19][C:20]1[N:30]([CH3:31])[C:26]2[CH:25]=[C:24]([N:32]3[CH2:37][CH2:36][N:35]([C:38]4[CH:39]=[CH:40][C:41]([C:44]([F:45])([F:47])[F:46])=[CH:42][CH:43]=4)[CH2:34][CH2:33]3)[C:23]([Cl:22])=[CH:29][C:27]=2[N:28]=1
参加物実験手順後処理出典と根拠反応ノート

参加物

4

反応物 3

HCID 12734Diisopropylcarbodiimide2 回HCID 679576795-Chloro-2-methylamino-4-(4-(4-trifluoromethylphenyl)piperazin-1-yl)anilineHCID 86646336N-(4-Chloro-3-isothiocyanatobenzyl)-1-(trifluoromethyl)cyclopropane carboxamide

生成物 1

HCID 57336792N-{4-Chloro-3-[5-chloro-1-methyl-6-(4-(4-trifluoromethylphenyl)piperazin-1-yl)-1H-benzimidazol-2-ylamino]-benzyl}-1-trifluoromethyl-cyclopropanamide

実験手順

N-(4-Chloro-3-isothiocyanatobenzyl)-1-trifluoromethyl-cyclopropane carboxamide (161 mg, 0.48 mmol) was added to the THF solution from step (a) above and the mixture was concentrated. DMF (2 mL) was added to the residue, the mixture was stirred at rt for 1 h and DIC (67 mg, 0.53 mmol) was added. The mixture was stirred at rt overnight, another portion of DIC (17 mg, 0.13 mmol) was added and the mixture was stirred at rt overnight. The mixture was concentrated and the residue was purified by column chromatography to give the title compound.

後処理

  1. concentrationwas concentrated
  2. additionDMF (2 mL) was added to the residue
  3. stirringThe mixture was stirred at rt overnight
  4. stirringthe mixture was stirred at rt overnight
  5. concentrationThe mixture was concentrated
  6. customthe residue was purified by column chromatography

出典と根拠

ORDレコード
ord-817d9a7eb9054bb3844d37a50dbd0abf
出典データセット
uspto-grants-2013_06
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US08466186B2

反応ノート

読み込み中…

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