反応式
Cl[C:2]1[C:11]2[C:6](=[CH:7][C:8]([O:12][CH3:13])=[CH:9][CH:10]=2)[C:5]([CH:14]=[O:15])=[C:4]([CH3:16])[N:3]=1.[CH:17]([C:20]1[CH:28]=[CH:27][C:26]2[NH:25][N:24]=[CH:23][C:22]=2[C:21]=1B(O)O)([CH3:19])[CH3:18].C([O-])([O-])=O.[Na+].[Na+]>O1CCOCC1.C1C=CC([P]([Pd]([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)[P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)=CC=1>[CH:17]([C:20]1[C:21]([C:2]2[C:11]3[C:6](=[CH:7][C:8]([O:12][CH3:13])=[CH:9][CH:10]=3)[C:5]([CH:14]=[O:15])=[C:4]([CH3:16])[N:3]=2)=[C:22]2[C:26](=[CH:27][CH:28]=1)[NH:25][N:24]=[CH:23]2)([CH3:19])[CH3:18]参加物
6
反応条件
- 温度
- 100 °C
実験手順
A mixture of 1-chloro-6-methoxy-3-methyl-isoquinoline-4-carbaldehyde (670 mg, 2.84 mmol), 5-isopropylindazole-4-boronic acid (580 mg, 2.84 mmol), Pd(PPh3)4 (164 mg, 0.14 mmol), and Na2CO3 (4.3 ml of 2M in H2O) in dioxane (15 ml) is heated for 18 h at 100° C. Usual work-up followed by flash chromatography over silica gel gives 342 mg of 1-(5-isopropyl-1H-indazol-4-yl)-6-methoxy-3-methyl-isoquinoline-4-carbaldehyde. 1H NMR (CDCl3) 10.9 (s, 1H), 8.68 (s, 1H), 7.65-7.37 (m, 3H), 7.42 (d, 1H), 7.01 (d, 1H), 4.01 (s, 3H), 3.15 (s, 3H), 2.71-2.63 (m, 1H), 1.22 (d, 3H), 1.10 (d, 3H).
出典と根拠
- ORDレコード
- ord-197d049a631b41df8dc1c6cbff52a61f
- 出典データセット
- uspto-grants-2011_03
- 特許番号
- US07915288B2
関連ノート
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