関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 1-(Benzyloxy)-3-bromobenzene | HCID 2756638 | — |
| 反応物 | 2-Methyl-6-(trifluoromethoxy)-1H-indole | HCID 12180669 | — |
| 試薬 | Sodium t-butoxide | HCID 23676156 | — |
| 触媒 | 2-(Di-tert-butylphosphino)biphenyl | HCID 2734215 | — |
| 触媒 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | 2-Methyl-1-(3-phenylmethoxyphenyl)-6-(trifluoromethoxy)indole | HCID 59216720 | 59.07% |
反応手順
EN04773-53, _Buchwald coupling, toluene and bromide_ The indole from 4773-25, 1-(benzyloxy)-3-bromobenzene,Pd2(dba)3, JohnPhos and KOtBu were dissolved in toluene. The mixture was warmed at 100 °C for 2h. Ca 60% conversion according to LCMS (product at 2.31 min). This conversion rate seemed faster than for the corresponding aryliodide. Big bacth was performed in 4773-54.
情報源と証拠
| 出典データセット | 750 AstraZeneca ELN dataset |
|---|
| ORD ID | ord-0addbbece6dc4ca2acdd8d8c9131d423 |
|---|
| 出典メモ | 750 AstraZeneca ELN dataset |
|---|
