Pyrrolidine → HCID 57955804、化合物

HRID 553235ノート

反応式

HRID 553235 の反応式
[C:1]([C:9]1[CH:25]=[CH:24][C:12]2[N:13]=[C:14]([C:16]3[CH:17]=[C:18]([C:21](O)=[O:22])[NH:19][CH:20]=3)[NH:15][C:11]=2[CH:10]=1)(=[O:8])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[NH:26]1[CH2:30][CH2:29][CH2:28][CH2:27]1.Cl.C(N=C=NCCCN(C)C)C.O.ON1C2C=CC=CC=2N=N1>CN(C)C=O.N1C=CC=CC=1.O>[C:1]([C:9]1[CH:25]=[CH:24][C:12]2[N:13]=[C:14]([C:16]3[CH:17]=[C:18]([C:21]([N:26]4[CH2:30][CH2:29][CH2:28][CH2:27]4)=[O:22])[NH:19][CH:20]=3)[NH:15][C:11]=2[CH:10]=1)(=[O:8])[C:2]1[CH:3]=[CH:4][CH:5]=[CH:6][CH:7]=1

参加物

8

反応物 4

HCID 31268PyrrolidineHCID 27239391,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 27960291-Hydroxybenzotriazole hydrateHCID 579557884-(6-Benzoyl-1H-benzimidazol-2-yl)-1H-pyrrole-2-carboxylic acid

生成物 1

HCID 57955804HCID 57955804、化合物収率 78.2%

試薬・触媒・溶媒 3

HCID 962Water溶媒HCID 1049Pyridine溶媒HCID 6228Dimethylformamide溶媒

反応条件

温度
80 °C

実験手順

The 4-(5-benzoylbenzimidazol-2-yl)-pyrrole-2-carboxylic acid (130 mg) obtained in Example 5 was dissolved in N,N-dimethylformamide (2 ml) and pyridine (2 ml). Pyrrolidine (56 mg), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (112 mg), and 1-hydroxybenzotriazole monohydrate (80 mg) were added and stirred overnight at 80° C. After the starting material was disappeared, the reaction mixture was allowed to cool to room temperature, and then added dropwise to water. The precipitate was collected by filtration, and dried in vacuo to afford ((4-(5-benzoylbenzimidazol-2-yl)-pyrrol-2-yl)-carbonyl)pyrrolidine (118 mg, 78%) as a red solid.

後処理

  1. temperatureto cool to room temperature
  2. filtrationThe precipitate was collected by filtration
  3. customdried in vacuo

出典と根拠

ORDレコード
ord-10fc7d3a6d6c42a9b9f4ab9a8f9ebf33
出典データセット
uspto-grants-2011_05
特許番号
US07951956B2

反応ノート

読み込み中…