HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Cesium carbonate → Methyl cis(+/-)-3-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-5-fluorobenzoate
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Cesium carbonate | HCID 10796 | — |
| Edukt | Binap, (A+-)- | HCID 634876 | — |
| Edukt | Methyl 3-chloro-5-fluorobenzoate | HCID 21942504 | — |
| Edukt | Benzyl cis(+/-)-[3-methoxypiperidin-4-yl]carbamate hydrochloride | HCID 86648698 | — |
| Katalysator | palladium(II) acetate | HCID 167845 | — |
| Produkt | Methyl cis(+/-)-3-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-5-fluorobenzoate | HCID 86648729 | 34,5% |
Reaktionsschritte
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%).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08536197B2 |
| Quelldatensatz | uspto-grants-2013_09 |
| ORD ID | ord-25c3092eb6694f7fb6faac504b527022 |
| Quellennotiz | uspto-grants-2013_09 |