Triethylamine → N-[4-Methoxy-3-(4-bromophenyl)aminocarbonyl-phenyl]-2-chloro-5-(2,2,2-trifluoro-1,1-dimethyl-ethyl)carbonylaminomethyl-benzamide

HRID 1846097ノート

反応式

HRID 1846097 の反応式
[F:1][C:2]([F:10])([F:9])[C:3]([CH3:8])([CH3:7])[C:4](O)=[O:5].[CH3:11][O:12][C:13]1[CH:18]=[CH:17][C:16]([NH:19][C:20](=[O:30])[C:21]2[CH:26]=[C:25]([CH2:27][NH2:28])[CH:24]=[CH:23][C:22]=2[Cl:29])=[CH:15][C:14]=1[C:31]([NH:33][C:34]1[CH:39]=[CH:38][C:37]([Br:40])=[CH:36][CH:35]=1)=[O:32].C(N(CC)CC)C.CN(C(ON1N=NC2C=CC=CC1=2)=[N+](C)C)C.[B-](F)(F)(F)F>CN(C=O)C>[CH3:11][O:12][C:13]1[CH:18]=[CH:17][C:16]([NH:19][C:20](=[O:30])[C:21]2[CH:26]=[C:25]([CH2:27][NH:28][C:4]([C:3]([CH3:8])([CH3:7])[C:2]([F:10])([F:9])[F:1])=[O:5])[CH:24]=[CH:23][C:22]=2[Cl:29])=[CH:15][C:14]=1[C:31]([NH:33][C:34]1[CH:35]=[CH:36][C:37]([Br:40])=[CH:38][CH:39]=1)=[O:32]

参加物

6

反応物 4

HCID 8471TriethylamineHCID 2733207O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborateHCID 198673673,3,3-Trifluoro-2,2-dimethylpropanoic acidHCID 67116388N-[4-Methoxy-3-(4-bromophenyl)aminocarbonyl-phenyl]-2-chloro-5-aminomethyl-benzamide

生成物 1

HCID 52919089N-[4-Methoxy-3-(4-bromophenyl)aminocarbonyl-phenyl]-2-chloro-5-(2,2,2-trifluoro-1,1-dimethyl-ethyl)carbonylaminomethyl-benzamide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒3 回

実験手順

To 1.0 mL of a 0.13 M solution of 3,3,3-trifluoro-2,2-dimethyl-propionic acid (0.13 mmol) in DMF was added 1.0 mL of a 0.1 M solution of N-[4-methoxy-3-(4-bromophenyl)aminocarbonyl-phenyl]-2-chloro-5-aminomethyl-benzamide (0.10 mmol) in DMF and triethylamine (70 μL, 0.50 mmol). Then 1.0 mL of a 0.115 M solution of TBTU (0.115 mmol) in DMF was added and the mixture was stirred overnight. The reaction mixture was directly purified via prep. HPLC to furnish the title compound.

後処理

  1. customThe reaction mixture was directly purified via prep

出典と根拠

ORDレコード
ord-c8d0b647482d47a1b88604b386905b31
出典データセット
uspto-grants-2015_02
特許番号
US08951999B2

反応ノート

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