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Triethylamine → 7-[3,5-Difluoro-4-(2-propynyloxy)benzoyl]-7-azabicyclo[4.1.0]heptane
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 7-Azabicyclo[4.1.0]heptane | HCID 549240 | — |
| 反応物 | 3,5-Difluoro-4-(2-propynyloxy)benzoyl chloride | HCID 57445696 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | 7-[3,5-Difluoro-4-(2-propynyloxy)benzoyl]-7-azabicyclo[4.1.0]heptane | HCID 57701178 | 62% |
反応手順
A mixture of 1.45 g of 7-azabicyclo[4.1.0]heptane, 2 ml of triethylamine and 3 ml of ethyl acetate was added dropwise to a mixture of 10 ml of ethyl acetate and 2.3 g of 3,5-difluoro-4-(2-propynyloxy)benzoic acid chloride under ice-cooling. The resulting mixture was stirred at room temperature for 4 hours. The reaction mixture was concentrated under reduced pressure. The residue was subjected to silica gel column chromatography to obtain 1.8 g of 7-[3,5-difluoro-4-(2-propynyloxy)benzoyl]-7-azabicyclo[4.1.0]heptane represented by the formula:
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07902400B2 |
| 出典データセット | uspto-grants-2011_03 |
| ORD ID | ord-a782385e680e44d1999e104da8b8b99f |
| 出典メモ | uspto-grants-2011_03 |