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Methanol → 7-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-1-(methoxymethyl)-3,4-dihydroquinolin-2(1H)-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Methanol | HCID 887 | — |
| 反応物 | Thionyl Chloride | HCID 24386 | — |
| 反応物 | Sodium Bicarbonate | HCID 516892 | — |
| 反応物 | N-Hydroxymethyl aripiprazole | HCID 58096483 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 7-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-1-(methoxymethyl)-3,4-dihydroquinolin-2(1H)-one | HCID 58096748 | 63% |
反応手順
To a mixture of hemiaminal A1 (2.0 g, 4.2 mmol) in dichloromethane (20 mL) was added thionyl chloride (1.5 mL, 12.6 mmol) and stirred for 2 h at room temperature. To the reaction mixture was added methanol (10 mL) and stirred a further 2 h. The reaction poured into NaHCO3 (aq) and extracted with dichloromethane. The organic phase dried over MgSO4, evaporated and the residue purified on silica eluting with 1:1:0.1 dichloromethane/ethyl acetate/methanol to give the title compound as a cream solid (1.3 g, 63%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08431576B2 |
| 出典データセット | uspto-grants-2013_04 |
| ORD ID | ord-5a05b82a700542d584650fd66e048c21 |
| 出典メモ | uspto-grants-2013_04 |