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3-Methyl-5-isoxazolecarboxylic acid → HCID 86759118、化合物
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3-Methyl-5-isoxazolecarboxylic acid | HCID 76947 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) | HCID 9886157 | — |
| 反応物 | HCID 69563649 | HCID 69563649 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | HCID 86759118 | HCID 86759118 | — |
反応手順
A solution of 5-methyl-isoxazole-3-carboxylic acid (65 mg) in dimethylformamide (30 ml) was treated successively with O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (190 mg), diisopropylethylamine (1 ml) and methyl (R) 3-amino-3-(1-boc-1,2,3,4-tetrahydro-quinolin-6-yl)-propionate (200 mg, Reference Example 14). After standing at room temperature overnight the mixture was evaporated to low bulk and the residue partitioned between ethyl acetate and dilute hydrochloric acid. The layers were separated and the organic layer was washed with sodium carbonate solution, dried, and evaporated. The residue was purified by flash chromatography to give the title compound as an orange gum, 310 mg.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06608084B1 |
| 出典データセット | uspto-grants-2003_08 |
| ORD ID | ord-e93d24a103e14d3699559b4987aab17e |
| 出典メモ | uspto-grants-2003_08 |