Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | Cyclopropanesulfonyl chloride | HCID 2760919 | — |
| Reactant | HCID 118431715 | HCID 118431715 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | HCID 118432133 | HCID 118432133 | 70.9% |
Reaction Steps
5-[3-(Piperazin-1-yl)-phenyl]-1-(2,4-difluoro-phenyl)-3-pentafluoroethyl-4,5-dihydro-1H-pyrazole hydrochloride (100.0 mg, 0.2 mmol) prepared in Step 1 of Example 96, triethylamine (143.0 uL, 1.02 mmol) and cyclopropanesulfonyl chloride (43.0 mg, 0.30 mmol) were added to dichloromethane (2.0 mL). The reaction mixture was stirred at room temperature for 18 hours, washed with distilled water, 1N hydrochloride, a saturated solution of sodium hydrogen carbonate, and brine, dried on anhydrous magnesium sulfate, and then concentrated under reduced pressure to give a yellow liquid residue. The resulting residue was purified by silica gel column chromatography (eluent: ethyl acetate/n-hexane=2/1) to give 80.0 mg of the titled compound as a yellow liquid.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US09376420B2 |
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| Source dataset | uspto-grants-2016_06 |
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| ORD ID | ord-0ce6b6dcbe064d52a368a37558028c02 |
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| Source note | uspto-grants-2016_06 |
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