Hydroxylamine → tert-Butyl N-{4-[amino(hydroxyimino)methyl]-2-fluorophenyl}glycinate
反応式
[C:1]([C:3]1[CH:8]=[CH:7][C:6]([NH:9][CH2:10][C:11]([O:13][C:14]([CH3:17])([CH3:16])[CH3:15])=[O:12])=[C:5]([F:18])[CH:4]=1)#[N:2].[NH2:19][OH:20]>CO>[NH2:2][C:1](=[N:19][OH:20])[C:3]1[CH:8]=[CH:7][C:6]([NH:9][CH2:10][C:11]([O:13][C:14]([CH3:15])([CH3:17])[CH3:16])=[O:12])=[C:5]([F:18])[CH:4]=1参加物
4
実験手順
tert-Butyl N-(4-cyano-2-fluorophenyl)glycinate obtained in Step 1 (290 mg; 1.16 mmol; 1 eq.) was dissolved in MeOH (1 mL) and hydroxylamine (0.34 mL; 5.79 mmol; 5 eq.) was added. The mixture was stirred at RT overnight. Solvents were evaporated off, affording the title product as an off-white solid, which was used further without purification (302 mg, 92%). HPLC (Method A) Rt 2.23 min (Purity: 74.2%).