Diisopropylethylamine → 3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(1-(diphenylmethyl)azetidin-3-yl)-1H-1,2,3-triazol-4-yl)-2-aminopyridine
反応式
[Cl:1][C:2]1[C:7]([F:8])=[CH:6][CH:5]=[C:4]([Cl:9])[C:3]=1[CH:10]([O:12][C:13]1[C:14]([NH2:21])=[N:15][CH:16]=[C:17]([C:19]#[CH:20])[CH:18]=1)[CH3:11].C(N(C(C)C)CC)(C)C.[C:31]1([CH:37]([C:45]2[CH:50]=[CH:49][CH:48]=[CH:47][CH:46]=2)[N:38]2[CH2:41][CH:40]([N:42]=[N+:43]=[N-:44])[CH2:39]2)[CH:36]=[CH:35][CH:34]=[CH:33][CH:32]=1>CO.[Cu](I)I>[Cl:1][C:2]1[C:7]([F:8])=[CH:6][CH:5]=[C:4]([Cl:9])[C:3]=1[CH:10]([O:12][C:13]1[C:14]([NH2:21])=[N:15][CH:16]=[C:17]([C:19]2[N:44]=[N:43][N:42]([CH:40]3[CH2:41][N:38]([CH:37]([C:31]4[CH:36]=[CH:35][CH:34]=[CH:33][CH:32]=4)[C:45]4[CH:50]=[CH:49][CH:48]=[CH:47][CH:46]=4)[CH2:39]3)[CH:20]=2)[CH:18]=1)[CH3:11]参加物
6
反応物 3
生成物 1
試薬・触媒・溶媒 2
実験手順
The compound 3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-ethynyl-2-aminopyridine (4.2 g, 12.62 mmol) was dissolved in methanol (40 mL), and diisopropylethylamine (8.36 g, 64.78 mmol), copper iodide (62 mg, 0.33 mmol) and 1-(diphenylmethyl)-3-azidoazetidine (3.34 g, 12.62 mmol) were added successively. The reaction was stirred overnight at room temperature. TLC test showed that the raw materials were completely reacted. The resultant mixture was concentrated under reduced pressure;
後処理
- customwere completely reacted
- concentrationThe resultant mixture was concentrated under reduced pressure
出典と根拠
- ORDレコード
- ord-b076a9776af34b5687b4bff2415888a9
- 出典データセット
- uspto-grants-2015_02
- 特許番号
- US08952002B2
反応ノート
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