Ammonia → 4-aminomethyl-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole
反応式
[O:1]1[CH2:6][CH2:5][CH2:4][CH2:3][CH:2]1[N:7]1[C:15]2[CH:14]=[CH:13][CH:12]=[C:11]([C:16]#[N:17])[C:10]=2[CH:9]=[N:8]1.N>CO.[Ni]>[O:1]1[CH2:6][CH2:5][CH2:4][CH2:3][CH:2]1[N:7]1[C:15]2[C:10](=[C:11]([CH2:16][NH2:17])[CH:12]=[CH:13][CH:14]=2)[CH:9]=[N:8]1参加物
5
実験手順
To a solution of 198 (430 mg, 1.89 mmol) in a 7N solution of NH3 in MeOH (20 mL) was added Raney nickel (50 mg), and the mixture was stirred under hydrogen (1 atm) at RT overnight. The Raney nickel was removed by filtration. The filtrate was concentrated to afford 340 mg (79%) of (1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-4-yl) methanamine (199) as yellow syrup: MS (ESI) m/z=232.2 [M+1]+.
後処理
- customThe Raney nickel was removed by filtration
- concentrationThe filtrate was concentrated
出典と根拠
- ORDレコード
- ord-5d1261c659a34763994c07971a5d2b95
- 出典データセット
- uspto-grants-2014_01
- 特許番号
- US08637537B2
反応ノート
読み込み中…