HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Triethylamine → 2-[1-(2-Chlorobenzoyl)-piperidin-4-ylmethoxy]-6-fluoro-benzonitrile
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Triethylamine | HCID 8471 | — |
| Edukt | 2-Chlorobenzoyl chloride | HCID 69110 | — |
| Edukt | 2-Fluoro-6-(piperidin-4-ylmethoxy)-benzonitrile hydrochloride | HCID 66924378 | — |
| Produkt | 2-[1-(2-Chlorobenzoyl)-piperidin-4-ylmethoxy]-6-fluoro-benzonitrile | HCID 66924235 | 86% |
Reaktionsschritte
A mixture of 2-fluoro-6-(piperidin-4-ylmethoxy)-benzonitrile hydrochloride (200 mg; 0.7 mmol) (Example 126, Step 3) was stirred at room temperature with 2-chlorobenzoyl chloride (129 mg; 0.7 mmol) and triethylamine (0.3 mL; 2.1 mmol) for 16 hours. Reaction was cooled and quenched with dilute HCl and mixture extracted with ethyl acetate (2×20 mL). Combined organics washed with water, saturated sodium bicarbonate, brine and dried over Na2SO4. Crude material was purified by chromatography using 0.5-2% methanol/DCM gradient to afford 2-[1-(2-chloro-benzoyl)-piperidin-4-ylmethoxy]-6-fluoro-benzonitrile as a white solid. (225 mg; 86% yield).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US07888366B2 |
| Quelldatensatz | uspto-grants-2011_02 |
| ORD ID | ord-2c244d55d0ae4463875669d0ff8f35cc |
| Quellennotiz | uspto-grants-2011_02 |