Hydrochloric Acid → 3-(4-(7-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-c]pyrimidin-5-yl)-1H-pyrazol-1-yl)-3-(piperidin-4-yl)propanenitrile
反応式
[C:1]([CH2:3][CH:4]([CH:25]1[CH2:30][CH2:29][N:28](C(OC(C)(C)C)=O)[CH2:27][CH2:26]1)[N:5]1[CH:9]=[C:8]([C:10]2[N:15]3[CH:16]=[CH:17][N:18]=[C:14]3[CH:13]=[C:12]([C:19]3[CH:20]=[N:21][N:22]([CH3:24])[CH:23]=3)[N:11]=2)[CH:7]=[N:6]1)#[N:2].C(Cl)[Cl:39].Cl.O1CCOCC1>>[ClH:39].[CH3:24][N:22]1[CH:23]=[C:19]([C:12]2[N:11]=[C:10]([C:8]3[CH:7]=[N:6][N:5]([CH:4]([CH:25]4[CH2:30][CH2:29][NH:28][CH2:27][CH2:26]4)[CH2:3][C:1]#[N:2])[CH:9]=3)[N:15]3[CH:16]=[CH:17][N:18]=[C:14]3[CH:13]=2)[CH:20]=[N:21]1.[CH3:24][N:22]1[CH:23]=[C:19]([C:12]2[N:11]=[C:10]([C:8]3[CH:7]=[N:6][N:5]([CH:4]([CH:25]4[CH2:30][CH2:29][NH:28][CH2:27][CH2:26]4)[CH2:3][C:1]#[N:2])[CH:9]=3)[N:15]3[CH:16]=[CH:17][N:18]=[C:14]3[CH:13]=2)[CH:20]=[N:21]1参加物
6
反応物 4
生成物 2
実験手順
Tert-butyl 4-(2-cyano-1-(4-(7-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-c]pyrimidin-5-yl)-1H-pyrazol-1-yl)ethyl)piperidine-1-carboxylate (59.4 mg, 0.118 mmol) was dissolved in DCM (592 μL, 0.118 mmol). To this was added 4N HCl in dioxane (296 μL, 1.18 mmol) and stirred at ambient temperature for 1 hour. Complete conversion was observed after 1 hour and the reaction mixture was concentrated to dryness to afford the HCl salt of 3-(4-(7-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-c]pyrimidin-5-yl)-1H-pyrazol-1-yl)-3-(piperidin-4-yl)propanenitrile (56.0 mg, 99.7% yield). MS (apci) m/z=402.3 (M+H).
後処理
- waitComplete conversion was observed after 1 hour
- concentrationthe reaction mixture was concentrated to dryness
出典と根拠
- ORDレコード
- ord-09a3f615c8234a4a8ba681533e67242a
- 出典データセット
- uspto-grants-2015_02
- 特許番号
- US08962596B2
反応ノート
読み込み中…