化工社化工社 化学情報印刷レポート · 研究参考用
Cesium carbonate → Methyl cis(+/-)-3-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-5-fluorobenzoate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | Binap, (A+-)- | HCID 634876 | — |
| 反応物 | Methyl 3-chloro-5-fluorobenzoate | HCID 21942504 | — |
| 反応物 | Benzyl cis(+/-)-[3-methoxypiperidin-4-yl]carbamate hydrochloride | HCID 86648698 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 生成物 | Methyl cis(+/-)-3-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-5-fluorobenzoate | HCID 86648729 | 34.5% |
反応手順
The same operation as in Example (42a) was performed using benzyl cis(±)-[3-methoxypiperidin-4-yl]carbamate hydrochloride obtained in Example (160a) (165 mg, 0.55 mmol), methyl 3-chloro-5-fluorobenzoate (103 mg, 0.55 mmol), palladium acetate (12.3 mg, 0.05 mmol), BINAP (68.3 mg, 0.11 mmol) and cesium carbonate (536 mg, 1.65 mmol), to obtain 79 mg of the title compound as a yellow oily substance (35%).
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-25c3092eb6694f7fb6faac504b527022 |
| 出典メモ | uspto-grants-2013_09 |