Tert-butyl 3-fluoro-4-(thiazol-4-yl)phenylcarbamate → 3-Fluoro-4-(thiazol-4-yl)benzenamine

HRID 559000ノート

反応式

HRID 559000 の反応式
[F:1][C:2]1[CH:3]=[C:4]([NH:13]C(=O)OC(C)(C)C)[CH:5]=[CH:6][C:7]=1[C:8]1[N:9]=[CH:10][S:11][CH:12]=1>C(Cl)Cl.C(O)(C(F)(F)F)=O>[F:1][C:2]1[CH:3]=[C:4]([NH2:13])[CH:5]=[CH:6][C:7]=1[C:8]1[N:9]=[CH:10][S:11][CH:12]=1

参加物

4

反応物 1

HCID 57471879Tert-butyl 3-fluoro-4-(thiazol-4-yl)phenylcarbamate

生成物 1

HCID 574718803-Fluoro-4-(thiazol-4-yl)benzenamine収率 81.1%

試薬・触媒・溶媒 2

HCID 6344Dichloromethane溶媒HCID 6422Trifluoroacetic acid溶媒

実験手順

A solution of tert-butyl 3-fluoro-4-(thiazol-4-yl)phenylcarbamate (270 mg, 0.92 mmol) in CH2Cl2 (2 mL) and TFA (4 mL) was stirred at room temperature for 60 min. It was then concentrated in vacuo. The residue was dissolved in CH2Cl2 (20 mL), which was washed with 5% NaHCO3, dried over Na2SO4, concentrated in vacuo to give 3-fluoro-4-(thiazol-4-yl)benzenamine (145 mg) as free base. MS 195.2 (M+H)

後処理

  1. concentrationIt was then concentrated in vacuo
  2. dissolutionThe residue was dissolved in CH2Cl2 (20 mL)
  3. washwhich was washed with 5% NaHCO3
  4. dry with materialdried over Na2SO4
  5. concentrationconcentrated in vacuo

出典と根拠

ORDレコード
ord-35921d9b1f1a401dba336db97e6f3342
出典データセット
uspto-grants-2011_11
特許番号
US08063058B2

反応ノート

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