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4-Methylmorpholine → Cyclophosphamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-Methylmorpholine | HCID 7972 | — |
| 反応物 | 3-Amino-1-propanol | HCID 9086 | — |
| 反応物 | Phosphorus oxychloride | HCID 24813 | — |
| 反応物 | Bis(2-chloroethyl)amine hydrochloride | HCID 522769 | — |
| 生成物 | Cyclophosphamide | HCID 2907 | — |
反応手順
3-aminopropanol (2.1 g, 0.028 mol) and N-methylmorpholine (12.9 eq) are placed into a three-necked flask and stirred at room temperature. After cooling the mixture in the flask, POCl3 (4.3 g, 0.028 mol) is slowly dropped into the mixture. After adding POCl3, the mixture in the flask is stirred at room temperature for 15 hours. After that, bis(2-chloroethyl)amine hydrochloride] (5 g, 0.028 mol) is added into the mixture in the flask. The mixture in the flask is heated to about 40° C. and stirred for 6 hours. (The conversion yield determined with HPLC is about 10.0%.)
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09115160B2 |
| 出典データセット | uspto-grants-2015_08 |
| ORD ID | ord-476edc016270404d86d4aa37bb45a02b |
| 出典メモ | uspto-grants-2015_08 |