反応式
C1CCNCC1.COc1ccc(N2CCN(C)CC2)c2c1CCN(C(=O)Cc1ccc(Br)cc1)C2>CC(C)(C)[O-].CC1(C)c2cccc(P(c3ccccc3)c3ccccc3)c2Oc2c(P(c3ccccc3)c3ccccc3)cccc21.COCCOC.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.[Na+].[Pd].[Pd]>COc1ccc(N2CCN(C)CC2)c2c1CCN(C(=O)Cc1ccc(N3CCCCC3)cc1)C2参加物
反応物 2
生成物 1
試薬・触媒・溶媒 4
反応条件
- 温度
- 100 °C
実験手順
2-(4-bromophenyl)-1-(5-methoxy-8-(4-methylpiperazin-1-yl)-3,4-dihydroisoquinolin-2(1H)-yl)ethanone (125 mg, 0.27 mmol),[Reactants],piperidine (23.22 mg, 0.27 mmol) was taken in a mixture of DME (5 mL):water (1.250 mL) under N2.The reaction mixture was purged under N2 for 10 min.Tris(dibenzylideneacetone)dipalladium (0) (14.98 mg, 0.02 mmol) was added to the above reaction.The resulting reaction was stirred for 3 hrs at reflux tempt.LCMS profile showed formation of required product.Reaction was cooled to rt,solvents was evapourated to dryness.Crude was diluted with DCM and water (min) and organic layer separated and concentrated .Purification was done on RP systme to get product 1-(5-methoxy-8-(4-methylpiperazin-1-yl)-3,4-dihydroisoquinolin-2(1H)-yl)-2-(4-(piperidin-1-yl)phenyl)ethanone as a solid.but the product was not submitted due to very less ammount.
出典と根拠
- ORDレコード
- ord-e759a68ff56d4b3bb4604b0f87a340c5
- 出典データセット
- 750 AstraZeneca ELN dataset
- 元リンク
- 出典を表示
関連ノート
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