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Picolinoyl Chloride Hydrochloride → Ethyl 1-(5-(2-(3-ethylureido)-7-(picolinamido)benzo[d]thiazol-5-yl)pyrimidin-2-yl)-4-methylpiperidine-4-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Picolinoyl Chloride Hydrochloride | HCID 135033 | — |
| 反応物 | Ethyl 1-(5-(7-amino-2-(3-ethylureido)benzo[d]thiazol-5-yl)pyrimidin-2-yl)-4-methylpiperidine-4-carboxylate | HCID 86664019 | — |
| 溶媒 | Pyridine | HCID 1049 | — |
| 生成物 | Ethyl 1-(5-(2-(3-ethylureido)-7-(picolinamido)benzo[d]thiazol-5-yl)pyrimidin-2-yl)-4-methylpiperidine-4-carboxylate | HCID 86664022 | 68% |
反応手順
Ethyl 1-(5-(7-amino-2-(3-ethylureido)benzo[d]thiazol-5-yl)pyrimidin-2-yl)-4-methylpiperidine-4-carboxylate (119 mg, 0.25 mmol) was dissolved in pyridine (2 ml) then picolinoyl chloride hydrochloride (58 mg, 0.33 mmol) was added with stirring and the reaction stirred at rt for 18 h. The pyridine was removed under reduced pressure and the residue triturated with water. The resulting solid was collected by filtration and dried to afford the crude product 100 mg (68%). This material was used directly in the next step without further purification.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09181234B2 |
| 出典データセット | uspto-grants-2015_11 |
| ORD ID | ord-277f3e01570845bfb258ebfe078f5730 |
| 出典メモ | uspto-grants-2015_11 |