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)-4-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-bromo-4-fluorobenzoate | HCID 7018022 | — |
| 反応物 | Benzyl cis(+/-)-[3-methoxypiperidin-4-yl]carbamate | HCID 86648490 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 生成物 | Methyl cis(+/-)-3-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-4-fluorobenzoate | HCID 86648744 | 61.5% |
反応手順
The same operation as in Example (42a) was performed using benzyl cis(±)-[3-methoxypiperidin-4-yl]carbamate obtained in Example (160a) (100 mg, 0.38 mmol), methyl 3-bromo-4-fluorobenzoate (264 mg, 1.13 mmol), palladium acetate (25.5 mg, 0.11 mmol), BINAP (141 mg, 0.23 mmol) and cesium carbonate (370 mg, 1.13 mmol), to obtain 97.4 mg of the title compound as a yellow oily substance. mass spectrum (ESI): m/z 417 (M+H)+.
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-255be12eceab457691cdb2f24f685f8f |
| 出典メモ | uspto-grants-2013_09 |