Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Potassium Iodide | HCID 4875 | — |
| Reactant | Potassium Carbonate | HCID 11430 | — |
| Reactant | 4,4-Difluoropiperidine hydrochloride | HCID 2758351 | — |
| Reactant | HCID 66975195 | HCID 66975195 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | HCID 66975454 | HCID 66975454 | 85.6% |
Reaction Steps
To a solution of tert-butyl (6R,7R)-6-{[(chloroacetyl)amino]methyl}-7-(4-chloro-3-fluorophenyl)-1,4-oxazepane-4-carboxylate (130 mg), 4,4-difluoropiperidine monohydrochloride (94 mg) and potassium iodide (9.91 mg) in THF (3.0 mL) was added potassium carbonate (248 mg), and the mixture was stirred at 60° C. overnight. To the reaction mixture was added distilled water, and the mixture was extracted with ethyl acetate. The extract was washed with distilled water and brine, and dried over anhydrous sodium sulfate, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel chromatography (hexane/ethyl acetate) to give the title compound (133 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08722662B2 |
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| Source dataset | uspto-grants-2014_05 |
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| ORD ID | ord-13557f0b01bc49c88e5e7ec57e349208 |
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| Source note | uspto-grants-2014_05 |
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