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Sodium Carbonate → Ethyl cis(+/-)-2-(4-{[(4-Chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-(dimethylamino)piperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Sodium Carbonate | HCID 10340 | — |
| 反応物 | Ethyl 2-bromo-4-methyl-1,3-thiazole-5-carboxylate | HCID 2824057 | — |
| 反応物 | 1,4-Dioxane hydrochloride | HCID 20443148 | — |
| 反応物 | tert-Butyl cis(+/-)-4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-(dimethylamino)-piperidine-1-carboxylate | HCID 86648777 | — |
| 生成物 | Ethyl cis(+/-)-2-(4-{[(4-Chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-(dimethylamino)piperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylate | HCID 86648778 | 90.2% |
反応手順
The same operation as in Example (196c) was performed using tert-butyl cis(±)-4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-(dimethylamino)-piperidine-1-carboxylate obtained in Example (200d) (104 mg, 0.260 mmol), 4 N hydrochloric acid/1,4-dioxane (2 mL), ethyl 2-bromo-4-methyl-1,3-thiazole-5-carboxylate (71.6 mg, 0.286 mmol) and sodium carbonate (551 mg, 5.20 mmol), to obtain 110 mg of the title compound (90%) as a pale yellow solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08536197B2 |
| 出典データセット | uspto-grants-2013_09 |
| ORD ID | ord-99208a47508147d6a803fef0cbfb6138 |
| 出典メモ | uspto-grants-2013_09 |