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Trifluoroacetic acid → 2-Amino-1-[4-(2-amino-2-cyclohexyl-acetyl)-6-(6-fluoro-1H-indol-3-yl)-hexahydro-pyrrolo[3,2-b]pyrrol-1-yl]-2-cyclohexyl-ethanone

HRID 1949661
ノート
印刷プレビュー

反応式

HRID 1949661 の反応式
C(OC(=O)[NH:7][CH:8]([CH:46]1[CH2:51][CH2:50][CH2:49][CH2:48][CH2:47]1)[C:9]([N:11]1[CH2:15][CH2:14][CH:13]2[N:16]([C:29](=[O:45])[CH:30]([NH:37]C(OC(C)(C)C)=O)[CH:31]3[CH2:36][CH2:35][CH2:34][CH2:33][CH2:32]3)[CH2:17][CH:18]([C:19]3[C:27]4[C:22](=[CH:23][C:24]([F:28])=[CH:25][CH:26]=4)[NH:21][CH:20]=3)[CH:12]12)=[O:10])(C)(C)C.C(O)(C(F)(F)F)=O>C(Cl)Cl>[NH2:7][CH:8]([CH:46]1[CH2:51][CH2:50][CH2:49][CH2:48][CH2:47]1)[C:9]([N:11]1[CH2:15][CH2:14][CH:13]2[N:16]([C:29](=[O:45])[CH:30]([NH2:37])[CH:31]3[CH2:36][CH2:35][CH2:34][CH2:33][CH2:32]3)[CH2:17][CH:18]([C:19]3[C:27]4[C:22](=[CH:23][C:24]([F:28])=[CH:25][CH:26]=4)[NH:21][CH:20]=3)[CH:12]12)=[O:10]
参加物実験手順後処理出典と根拠反応ノート

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 67407842{2-[4-(2-tert-Butoxycarbonylamino-2-cyclohexyl-acetyl)-6-(6-fluoro-1H-indol-3-yl)-hexahydro-pyrrolo[3,2-b]pyrrol-1-yl]-1-cyclohexyl-2-oxo-ethyl}-carbamic acid tert-butyl ester

生成物 1

HCID 674121332-Amino-1-[4-(2-amino-2-cyclohexyl-acetyl)-6-(6-fluoro-1H-indol-3-yl)-hexahydro-pyrrolo[3,2-b]pyrrol-1-yl]-2-cyclohexyl-ethanone収率 78.6%

試薬・触媒・溶媒 1

HCID 6344
Dichloromethane
溶媒

実験手順

To a solution containing 121 (370 mg, 0.51 mmol) in DCM (10 mL) at 0° C. was added TFA (4 mL). After 2 h, the reaction mixture was concentrated in vacuo. The residue was dissolved in DCM and the organic solution was washed successively with saturated aqueous NaHCO3 and brine, dried over anhydrous Na2SO4, filtered, and concentrated to afford 210 mg of 122 which was used without further purification. Mass spectrum, m/z [523.3] (M)+.

後処理

  1. concentrationthe reaction mixture was concentrated in vacuo
  2. dissolutionThe residue was dissolved in DCM
  3. washthe organic solution was washed successively with saturated aqueous NaHCO3 and brine
  4. dry with materialdried over anhydrous Na2SO4
  5. filtrationfiltered
  6. concentrationconcentrated

出典と根拠

ORDレコード
ord-1dfa6b6634fe417db0aba7886e7f1303
出典データセット
uspto-grants-2013_03
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US08399683B2

反応ノート

読み込み中…

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