関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Nitrogen mustard hydrochloride | HCID 5935 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 2-Amino-1,3-thiazole-5-carbaldehyde | HCID 2737798 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 2-(4-Methylpiperazin-1-yl)-1,3-thiazole-5-carbaldehyde | HCID 1490234 | 50.9% |
反応手順
In a 25 ml flask are added 0.5 g of 2-aminothiazole-5-carboxaldehyde, 1.35 g of K2CO3 in 5 ml of DMF. After dissolution, 0.901 g of 2-chloro-N-(2-chloroethyl)-N-methylethanamine hydrochloride are added. The mixture is left at room temperature for 1 h then heated to 90° C. for 5 h. Next, the mixture is evaporated, dissolved in 100 ml of water, and the aqueous phase is extracted three times with ethyl acetate. The organic phases are combined, washed with sodium chloride saturated solution, dried over sodium sulfate, filtered, and evaporated to yield 420 mg (50%) of 2-(4-methylpiperazin-1-yl)thiazole-5-carboxaldehyde.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08889711B2 |
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| 出典データセット | uspto-grants-2014_11 |
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| ORD ID | ord-39af4352341447feae9be1a7f75ba4c3 |
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| 出典メモ | uspto-grants-2014_11 |
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