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HRID 14997作成日：2026年10月25日
Diisopropylethylamine → 2-(5,5-Dioxo-5,10-dihydrophenothiazin-2-yl)-n-(1-methyl-1h-pyrazol-3-yl)-3-(tetrahydropyran-4-yl)propionamide
https://huagongshe.com/reaction/14997
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 1-Methyl-3-aminopyrazole | HCID 137254 | — |
| 反応物 | HOAt | HCID 181649 | — |
| 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 | 2-(5,5-Dioxo-5,10-dihydrophenothiazin-2-yl)-3-(tetrahydropyran-4-yl)propionic acid | HCID 58024229 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | 2-(5,5-Dioxo-5,10-dihydrophenothiazin-2-yl)-n-(1-methyl-1h-pyrazol-3-yl)-3-(tetrahydropyran-4-yl)propionamide | HCID 58024260 | — |
反応手順
600 mg of 2-(5,5-dioxo-5,10-dihydrophenothiazin-2-yl)-3-(tetrahydropyran-4-yl)propionic acid, 120 mg of commercially available 1-methyl-1H-pyrazole-3-amine and 729 μl of N,N-diisopropylethylamine are dissolved in 5 ml of dimethylformamide. 561 mg of HATU and 200 mg of HOAT are added, and the mixture is stirred at room temperature for two hours. The reaction mixture is then diluted by addition of 200 ml of ethyl acetate and washed three times with in each case 50 ml of water and saturated sodium chloride solution. The organic phase is dried over MgSO4, and the solvent is then removed under reduced pressure. The residue is purified by RP-HPLC. This gives 200 mg of 2-(5,5-dioxo-5,10-dihydrophenothiazin-2-yl)-N-(11-methyl-1H-pyrazol-3-yl)-3-(tetrahydropyran-4-yl)propionamide as a colorless lyophilisate.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07732440B2 |
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| 出典データセット | uspto-grants-2010_06 |
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| ORD ID | ord-6d934af18b0a4f2baa267241da828b8e |
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| 出典メモ | uspto-grants-2010_06 |
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