Tert-butyl 3-((4-fluoro-2-methylphenyl)(methyl)amino)azetidine-1-carboxylate → N-(4-fluoro-2-methylphenyl)-N-methylazetidin-3-amine
反応式
[F:1][C:2]1[CH:7]=[CH:6][C:5]([N:8]([CH3:20])[CH:9]2[CH2:12][N:11](C(OC(C)(C)C)=O)[CH2:10]2)=[C:4]([CH3:21])[CH:3]=1>ClCCl>[F:1][C:2]1[CH:7]=[CH:6][C:5]([N:8]([CH3:20])[CH:9]2[CH2:12][NH:11][CH2:10]2)=[C:4]([CH3:21])[CH:3]=1参加物
3
実験手順
To an ice cooled solution of tert-butyl 3-((4-fluoro-2-methylphenyl)(methyl)amino)azetidine-1-carboxylate (D33) 8170 mg, 0.577 mmol) in dichloromethane (1 ml) trifluoroacetic acid/dichloromethane (3/1 ml) was added and the resulting mixture was stirred at room temperature for 1 h. Solvents were evaporated under vacuo and the residue was purified by SPE-SCX cartridge (10 g) eluting with methanol and 2N ammonia in methanol. Ammonia fractions were evaporated in vacuo to afford the title compound (D56) (110 mg)