Diisopropylethylamine → N-{4-Chloro-3-[6-chloro-5-(3,3-difluoropyrrolidin-1-yl)-1H-benzo[d]imidazol-2-ylamino]benzyl}-2,2-dimethyl-propionamide

HRID 1258637ノート

反応式

HRID 1258637 の反応式
Cl.Cl.[Cl:3][C:4]1[CH:5]=[C:6]([NH2:18])[C:7]([NH2:17])=[CH:8][C:9]=1[N:10]1[CH2:14][CH2:13][C:12]([F:16])([F:15])[CH2:11]1.[Cl:19][C:20]1[CH:33]=[CH:32][C:23]([CH2:24][NH:25][C:26](=[O:31])[C:27]([CH3:30])([CH3:29])[CH3:28])=[CH:22][C:21]=1[N:34]=[C:35]=S.CCN(C(C)C)C(C)C>CC#N>[Cl:19][C:20]1[CH:33]=[CH:32][C:23]([CH2:24][NH:25][C:26](=[O:31])[C:27]([CH3:30])([CH3:29])[CH3:28])=[CH:22][C:21]=1[NH:34][C:35]1[NH:18][C:6]2[CH:5]=[C:4]([Cl:3])[C:9]([N:10]3[CH2:14][CH2:13][C:12]([F:16])([F:15])[CH2:11]3)=[CH:8][C:7]=2[N:17]=1

参加物

5

反応物 3

HCID 81531DiisopropylethylamineHCID 679580194-Chloro-5-(3,3-difluoropyrrolidin-1-yl)benzene-1,2-diamine dihydrochlorideHCID 86646343HCID 86646343、化合物

生成物 1

HCID 67975174N-{4-Chloro-3-[6-chloro-5-(3,3-difluoropyrrolidin-1-yl)-1H-benzo[d]imidazol-2-ylamino]benzyl}-2,2-dimethyl-propionamide

試薬・触媒・溶媒 1

HCID 6342Acetonitrile溶媒

実験手順

4-Chloro-5-(3,3-difluoropyrrolidin-1-yl)benzene-1,2-diamine dihydrochloride (340 mg, 1.1 mmol) was added to N-(4-chloro-3-isothiocyanatobenzyl)-2,2-dimethyl-propionamide (300 mg, 1.1 mmol) in MeCN (10 mL) and stirred at rt overnight. After addition of DIPEA (0.41 μL, 2.3 mmol) the reaction mixture was stirred at rt for 4.5 h. The mixture was concentrated. The crude was purified by chromatography to give the sub-title compound.

後処理

  1. stirringwas stirred at rt for 4.5 h
  2. concentrationThe mixture was concentrated
  3. customThe crude was purified by chromatography

出典と根拠

ORDレコード
ord-4eb431c42b41453b98e0e184db763666
出典データセット
uspto-grants-2013_06
特許番号
US08466186B2

反応ノート

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