Trifluoroacetic acid → {6-Fluoro-5-[2-methyl-4-(2,3,4,5-tetrahydrobenzo[b]azepine-1-carbonyl)benzylcarbamoyl]-2-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]diazepin-1-yl}-acetic acid

HRID 558951ノート

反応式

HRID 558951 の反応式
C([O:5][C:6](=[O:45])[CH2:7][N:8]1[C:14](=[O:15])[CH2:13][CH2:12][N:11]([C:16](=[O:39])[NH:17][CH2:18][C:19]2[CH:24]=[CH:23][C:22]([C:25]([N:27]3[CH2:33][CH2:32][CH2:31][CH2:30][C:29]4[CH:34]=[CH:35][CH:36]=[CH:37][C:28]3=4)=[O:26])=[CH:21][C:20]=2[CH3:38])[C:10]2[C:40]([F:44])=[CH:41][CH:42]=[CH:43][C:9]1=2)(C)(C)C.FC(F)(F)C(O)=O>ClCCl>[F:44][C:40]1[C:10]2[N:11]([C:16](=[O:39])[NH:17][CH2:18][C:19]3[CH:24]=[CH:23][C:22]([C:25]([N:27]4[CH2:33][CH2:32][CH2:31][CH2:30][C:29]5[CH:34]=[CH:35][CH:36]=[CH:37][C:28]4=5)=[O:26])=[CH:21][C:20]=3[CH3:38])[CH2:12][CH2:13][C:14](=[O:15])[N:8]([CH2:7][C:6]([OH:45])=[O:5])[C:9]=2[CH:43]=[CH:42][CH:41]=1

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 59807185{6-Fluoro-5-[2-methyl-4-(2,3,4,5-tetrahydrobenzo[b]azepine-1-carbonyl)-benzylcarbamoyl]-2-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]diazepin-1-yl}acetic Acid Tert-Butyl Ester

生成物 1

HCID 11699686{6-Fluoro-5-[2-methyl-4-(2,3,4,5-tetrahydrobenzo[b]azepine-1-carbonyl)benzylcarbamoyl]-2-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]diazepin-1-yl}-acetic acid

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

To a solution of {6-fluoro-5-[2-methyl-4-(2,3,4,5-tetrahydrobenzo[b]azepine-1-carbonyl)benzylcabamoyl]-2-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]diazepin-1-yl]acetic acid tert-butyl ester from Example 1 (250 mg, 0.40 mmol) in dichloromethane (8 ml) was added trifluoroacetic acid (8 ml). The mixture was stirred for 90 min and evaporated in vacuo and azeotroped with toluene to give an off-white solid; yield 220 mg, 99%.

後処理

  1. customevaporated in vacuo
  2. customazeotroped with toluene
  3. customto give an off-white solid

出典と根拠

ORDレコード
ord-18573718bc5d4498920c438613b81368
出典データセット
uspto-grants-2011_11
特許番号
US08063038B2

反応ノート

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