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

HRID 499834ノート

反応式

HRID 499834 の反応式
[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

参加物

6

反応物 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

生成物 1

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

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

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).

後処理

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

出典と根拠

ORDレコード
ord-d3bfbbe0bd634f3ebf06a39d91691100
出典データセット
uspto-grants-2010_08
特許番号
US07767697B2

反応ノート

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