関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Piperidine | HCID 8082 | — |
| 反応物 | 2-(4-Bromo-phenyl)-1-[5-methoxy-8-(4-methyl-piperazin-1-yl)-3,4-dihydro-1H-isoquinolin-2-yl]-ethanone | HCID 69448388 | — |
| 試薬 | Sodium t-butoxide | HCID 23676156 | — |
| 触媒 | 1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine) | HCID 636044 | — |
| 触媒 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 溶媒 | 1,2-Dimethoxyethane | HCID 8071 | — |
| 生成物 | 1-[5-Methoxy-8-(4-methyl-piperazin-1-yl)-3,4-dihydro-1H-isoquinolin-2-yl]-2-(4-piperidin-1-yl-phenyl)-ethanone | HCID 58794054 | 0% |
反応手順
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.
情報源と証拠
| 出典データセット | 750 AstraZeneca ELN dataset |
|---|
| ORD ID | ord-e759a68ff56d4b3bb4604b0f87a340c5 |
|---|
| 出典メモ | 750 AstraZeneca ELN dataset |
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