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Potassium Carbonate → (1-Thiiranylmethyl-piperidin-4-yl)-carbamic acid tert-butyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | Epithiochlorohydrin | HCID 18588 | — |
| 反応物 | 4-(N-Boc-amino)piperidine | HCID 723833 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | (1-Thiiranylmethyl-piperidin-4-yl)-carbamic acid tert-butyl ester | HCID 86662008 | 114% |
反応手順
Epithiochlorohydrine (268 mg, 2.40 mmol, 1.0 eq) is added at room temperature to a stirred solution of piperidin-4-yl-carbamic acid tert-butyl ester (500 mg, 2.40 mmol, 1.0 eq) in N,N-dimethylformamide (15 mL), followed by potassium carbonate (335 mg, 2.40 mmol, 1.0 eq). After 24 hours stirring at room temperature, solvent is evaporated and the residue is extracted with dichloromethane (3×20 mL) and water (20 mL). The combined organic layers are dried over sodium sulfate, filtered and concentrated to afford (1-thiiranylmethyl-piperidin-4-yl)-carbamic acid tert-butyl ester as a white solid (745 mg, 57% yield).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08716280B2 |
| 出典データセット | uspto-grants-2014_05 |
| ORD ID | ord-1f08cec811ef4ec28998c6ab2d44f353 |
| 出典メモ | uspto-grants-2014_05 |