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Triethylamine → N-((1-(4-(2-oxopyridin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)-1H-indole-5-carboxamide

HRID 2357844
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HRID 2357844 반응식
[NH:1]1[C:9]2[C:4](=[CH:5][C:6]([C:10]([OH:12])=O)=[CH:7][CH:8]=2)[CH:3]=[CH:2]1.C(N(CC)CC)C.F[P-](F)(F)(F)(F)F.N1(O[P+](N(C)C)(N(C)C)N(C)C)C2C=CC=CC=2N=N1.Cl.[NH2:48][CH2:49][C:50]1[N:51]=[CH:52][N:53]([C:55]2[CH:60]=[CH:59][C:58]([N:61]3[CH:66]=[CH:65][CH:64]=[CH:63][C:62]3=[O:67])=[CH:57][CH:56]=2)[CH:54]=1>CN(C=O)C>[O:67]=[C:62]1[CH:63]=[CH:64][CH:65]=[CH:66][N:61]1[C:58]1[CH:59]=[CH:60][C:55]([N:53]2[CH:54]=[C:50]([CH2:49][NH:48][C:10]([C:6]3[CH:5]=[C:4]4[C:9](=[CH:8][CH:7]=3)[NH:1][CH:2]=[CH:3]4)=[O:12])[N:51]=[CH:52]2)=[CH:56][CH:57]=1
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참가 물질

6

반응물 4

HCID 8471TriethylamineHCID 742801H-Indole-5-Carboxylic AcidHCID 151348Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphateHCID 669741011-(4-(4-(aminomethyl)-1H-imidazol-1-yl)phenyl)pyridin-2(1H)-one hydrochloride

생성물 1

HCID 24760449N-((1-(4-(2-oxopyridin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)-1H-indole-5-carboxamide수율 40.7%

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

To a solution of indole-5-carboxylic acid (40 mg, 0.25 mmol) and triethylamine (0.150 mL, 1.08 mmol) in DMF (2 mL), BOP (135 mg, 0.30 mmol) was added. After 5 min of stirring, 1-(4-(4-(aminomethyl)-1H-imidazol-1-yl)phenyl)pyridin-2(1H)-one hydrochloride (53 mg, 0.18 mmol) was added. The mixture was stirred at room temperature overnight. It was then purified by HPLC to give the titled compound (30 mg). MS 410.2 (M+H).

후처리

  1. stirringThe mixture was stirred at room temperature overnight
  2. customIt was then purified by HPLC

출처 및 근거

ORD 기록
ord-085b854eb4944acd97277cc2d08ab75e
출처 데이터셋
uspto-grants-2010_07
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07763608B2

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