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Cesium carbonate → Ethyl cis(+/-)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)pyridine-3-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | Ethyl 5-bromopyridine-3-carboxylate | HCID 140785 | — |
| 反応物 | Binap, (A+-)- | HCID 634876 | — |
| 反応物 | Benzyl cis(+/-)-[3-methoxypiperidin-4-yl]carbamate hydrochloride | HCID 86648698 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 生成物 | Ethyl cis(+/-)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)pyridine-3-carboxylate | HCID 86648702 | 51.2% |
反応手順
The same operation as in Example (160b) was performed using benzyl cis(±)-[3-methoxypiperidin-4-yl]carbamate hydrochloride obtained in Example (160a) (832 mg, 2.76 mmol), ethyl 5-bromopyridine-3-carboxylate (530 mg, 2.3 mmol), palladium acetate (51.72 mg, 0.23 mmol), BINAP (286.89 mg, 0.46 mmol), and cesium carbonate (2.25 g, 6.91 mmol), to obtain 487 mg of the title compound as a yellow oily substance.
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-f7084e78cd4e493192a1becde05d7c28 |
| 出典メモ | uspto-grants-2013_09 |