Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|
| Edukt | Sodium Iodide | HCID 5238 | — |
| Edukt | Potassium Carbonate | HCID 11430 | — |
| Edukt | 4-Chlorobenzhydryl chloride | HCID 241584 | — |
| Edukt | HCID 86703762 | HCID 86703762 | — |
| Lösungsmittel | Acetonitrile | HCID 6342 | — |
| Lösungsmittel | Ethyl Acetate | HCID 8857 | — |
| Lösungsmittel | Sodium chloride; water | HCID 57417360 | — |
| Produkt | HCID 86703761 | HCID 86703761 | 50% |
Reaktionsschritte
A mixture of methyl 4-(azetidin-3-ylmethoxy)-5-cyclopropyl-2-fluorobenzoate (58 mg, 0.21 mmol), 1-chloro-4-(chloro(phenyl)methyl)benzene (74 mg, 0.31 mmol), potassium carbonate (86 mg, 0.62 mmol) and sodium iodide (32 mg, 0.21 mmol) in MeCN (10 mL) was stirred at 80° C. for 16 h. The reaction mixture was diluted with EtOAc (100 mL) and brine (50 mL). The organic layer was separated and washed with brine (50×2 mL), dried over anhydrous sodium sulfate, filtered and concentrated. The residue was purified by silica gel chromatography (eluting with petroleum ether/EtOAc=4/1) to give the target compound (50 mg, 50%) as a pale yellow oil. LCMS (ESI) m/z: 480.1 [M+H].
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patentnummer | US08952169B2 |
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| Quelldatensatz | uspto-grants-2015_02 |
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| ORD ID | ord-03ff19756b6c4eefb8063a25a595a1f7 |
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| Quellennotiz | uspto-grants-2015_02 |
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