Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Sodium Iodide | HCID 5238 | — |
| Reactant | Potassium Carbonate | HCID 11430 | — |
| Reactant | 2-Bromo-3-(2,4-difluorophenyl)-6-hydroxy-1H-inden-1-one | HCID 70307437 | — |
| Reactant | HCID 88266393 | HCID 88266393 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | HCID 70312831 | HCID 70312831 | 66% |
Reaction Steps
To a solution of 2-bromo-3-(2,4-difluorophenyl)-6-hydroxy-1H-inden-1-one (500 mg, 1.48 mmol) obtained in Step 5 of Example 82 in DMF was added K2CO3(3 eq), 3-[4-(methylsulfonyl)piperazin-1-yl]propyl methanesulfonate (669 mg, 2.23 mmol, 1.5 eq), and NaI (0.3 eq) sequentially. The mixture was heated to 60° C. for 16 h. The reaction mixture was quenched with H2O and extracted with EtOAc. The organic layer was washed with H2O and brine, dried over MgSO4, and concentrated in vacuo. The residue was purified by silica gel column chromatography (2% MeOH/CH2Cl2) to obtain the title compound (66%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US08877747B2 |
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| Source dataset | uspto-grants-2014_11 |
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| ORD ID | ord-cea1fe93e2f241bda90dff6521d838f3 |
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| Source note | uspto-grants-2014_11 |
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