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Triethylamine → (4-(1-(4-Bromobenzyl)-5-methoxy-2-methyl-1H-indol-3-yl)-3-methylbutanoyl)-4-methylpiperazine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 1-Methylpiperazine | HCID 53167 | — |
| 反応物 | Diethyl cyanophosphonate | HCID 76257 | — |
| 反応物 | 4-(1-(4-Bromobenzyl)-5-methoxy-2-methyl-1H-indol-3-yl)-3-methylbutanoic acid | HCID 9867333 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | (4-(1-(4-Bromobenzyl)-5-methoxy-2-methyl-1H-indol-3-yl)-3-methylbutanoyl)-4-methylpiperazine | HCID 19041728 | — |
反応手順
To a solution of the acid from Example 7, Step 6 (300 mg) in DMF (4 mL) was added triethylamine (0.13 mL), diethyl cyanophosphonate (0.13 mL) and 1-methylpiperazine (0.08 mL) at r.t. After 4 h the reaction mixture was diluted with EtOAc and the organic phase was washed with HCl 1M, 5% aqueous NaHCO3 and brine, dried (MgSO4) and evaporated. Flash chromatography of the residue (silica gel; CH2Cl2 /MeOH, 95:5) afforded the title compound as a white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05639780 |
| 出典データセット | uspto-grants-1997_06 |
| ORD ID | ord-1b334975065b430cb5d670230529c4ef |
| 出典メモ | uspto-grants-1997_06 |