Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Phenetole | HCID 7674 | — |
| Reactant | Oxalyl chloride | HCID 65578 | — |
| Reactant | Aluminum(III) Chloride | HCID 6451240 | — |
| Reactant | HCID 71076950 | HCID 71076950 | — |
| Reactant | HCID 86714064 | HCID 86714064 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | HCID 71110860 | HCID 71110860 | 79.8% |
Reaction Steps
After dissolving crude 7-bromo-4-chlorobenzo[b]thiophene-5-carboxylic acid 97 (847 mg, 2.91 mmol) in CH2Cl2, (COCl)2 (0.49 mL, 5.82 mmol) and catalytic amount DMF was added carefully at 0° C. The resulting solution was stirred overnight at room temperature. The volatiles were evaporated under reduced pressure and dried in vacuo. The crude compound was used for the next step without further purification. To a solution of crude 7-bromo-4-chlorobenzo[b]thiophene-5-carbonyl chloride in CH2Cl2 (50 mL) was added ethoxybenzene (462 mg, 3.78 mmol) and AlCl3 (464 mg, 3.49 mmol) at 0° C. After warming the reaction mixture up to room temperature, it was stirred for 4 hours. The resulting compound was quenched with aq. NH4Cl solution and the normal work-up with EtOAc was conducted. Purification by silica gel chromatography gave the title compound (917 mg, 79.8%) as an off-white solid.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US09034921B2 |
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| Source dataset | uspto-grants-2015_05 |
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| ORD ID | ord-7b3d7bf142924e24bc38788de504e5d7 |
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| Source note | uspto-grants-2015_05 |
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