Pyrrolidine → HCID 57955804, 화합물

HRID 553235노트

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HRID 553235 반응식
[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

참가 물질

8

반응물 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

생성물 1

HCID 57955804HCID 57955804, 화합물수율 78.2%

시약·촉매·용매 3

HCID 962Water용매HCID 1049Pyridine용매HCID 6228Dimethylformamide용매

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온도
80 °C

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-10fc7d3a6d6c42a9b9f4ab9a8f9ebf33
출처 데이터셋
uspto-grants-2011_05
특허 번호
US07951956B2

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