HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Cesium carbonate → Methyl cis(+/-)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-3-methylthiophene-2-carboxylate
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Cesium carbonate | HCID 10796 | — |
| Edukt | Binap, (A+-)- | HCID 634876 | — |
| Edukt | Methyl 5-bromo-3-methylthiophene-2-carboxylate | HCID 53438912 | — |
| Edukt | Benzyl cis(+/-)-[3-methoxypiperidin-4-yl]carbamate | HCID 86648490 | — |
| Katalysator | palladium(II) acetate | HCID 167845 | — |
| Produkt | Methyl cis(+/-)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-3-methylthiophene-2-carboxylate | HCID 86648826 | 23,6% |
Reaktionsschritte
The same operation as in Example (244b) was performed using methyl 5-bromo-3-methylthiophene-2-carboxylate obtained in Example (245a) (218 mg, 0.93 mmol), benzyl cis(±)-(3-methoxypiperidin-4-yl)-carbamate obtained in Example (40b) (270 mg, 1.02 mmol), palladium acetate (42 mg, 0.19 mmol), BINAP (115 mg, 0.19 mmol) and cesium carbonate (423 mg, 1.30 mmol), to obtain 92 mg of the title compound as a yellow oily substance (24%).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08536197B2 |
| Quelldatensatz | uspto-grants-2013_09 |
| ORD ID | ord-9f771965f51343cb83a6d86cf4b28fbe |
| Quellennotiz | uspto-grants-2013_09 |