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HRID 1162787作成日:2026年10月24日
Formic Acid → 2-(2-(4-(2-(Methylamino)ethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide
https://huagongshe.com/ja/reaction/1162787
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
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| 反応物 | Formic Acid | HCID 284 | — |
| 反応物 | Methylamine | HCID 6329 | — |
| 反応物 | 2-(1-(2-(3-carbamoyl-4,5,6,7-tetrahydrobenzo[b]thiophen-2-ylamino)-2-oxoethyl)-3-(trifluoromethyl)1H-pyrazol-4-yl)ethyl methanesulfonate | HCID 59520461 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 2-(2-(4-(2-(Methylamino)ethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide | HCID 59520466 | 13.1% |
反応手順
The 2-(1-(2-(3-carbamoyl-4,5,6,7-tetrahydrobenzo[b]thiophen-2-ylamino)-2-oxoethyl)-3-(trifluoromethyl)1H-pyrazol-4-yl)ethyl methanesulfonate (30 mg, 0.061 mmol) was dissolved in DMF (1 mL) and methylamine (2 M in THF, 1 mL, 2 mmol) added. The reaction mixture was heated at 120° C. for 5 min in the microwave. The THF was removed in vacuo and the reaction mixture filtered and purified by preparative reverse phase HPLC to give the formic acid salt of the desired product (3.6 mg, 0.008 mmol, 12%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07820707B2 |
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| 出典データセット | uspto-grants-2010_10 |
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| ORD ID | ord-4fcfae59353649e49cdea4ee85fd3982 |
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| 出典メモ | uspto-grants-2010_10 |
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