関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | N-Phthaloylglycine | HCID 20825 | — |
| 反応物 | 1,1'-Carbonyldiimidazole | HCID 68263 | — |
| 反応物 | N'-Hydroxycyclopropanecarboximidamide | HCID 2794666 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | N-[(3-cyclopropyl-1,2,4-oxadiazol-5-yl)methyl]phthalimide | HCID 22713498 | — |
反応手順
N-Phthaloylglycine (90.7 g, 442 mmol) was dissolved in portions (because of clumping) in DMF (500 mL). 1,1′-Carbonyldiimidazole (78.9 g, 486 mmrol) was added in portions (attention CO evolution). The resulting suspension was heated at 80° C. for 20 min. and then cooled to rt, then cyclopropanecarboxamidoxime 1 added and then heated at 110° C. for 2 h. The solution was cooled to rt, then poured into water (4 L), stirred for 15 min, filtered, washed with water (400 mL) and (fried. Yield: 104 g (87%). Mp 115° C. m/z 269 (M).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US06743789B2 |
|---|
| 出典データセット | uspto-grants-2004_06 |
|---|
| ORD ID | ord-df8c010fc5e341939ff74e831a8364c9 |
|---|
| 出典メモ | uspto-grants-2004_06 |
|---|
