HuagongsheHuagongshe Chemistry Print Report · For research reference only
Trifluoroacetic acid → 3-[Cyclopropyl(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indole
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Trifluoroacetic acid | HCID 6422 | — |
| Reactant | Cyclopropyl(2,2-difluoro-1,3-benzodioxol-5-yl)methanol | HCID 58392116 | — |
| Reactant | 5-Fluoro-7-[(methylsulfonyl)methyl]-1H-indole | HCID 58392318 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | 3-[Cyclopropyl(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indole | HCID 44595238 | — |
Reaction Steps
100 mg (0.44 mmol) of the compound from Example 157A and 0.04 ml (0.53 mmol) of trifluoroacetic acid were added to 100 mg (0.44 mmol) of the compound from Example 87A in 5 ml of dichloromethane. The reaction mixture was stirred at RT for 45 min, the solvent was removed in vacuo, and the crude product was then purified by preparative HPLC (mobile phase: acetonitrile/water gradient). 151 mg (78% of theory) of the title compound were obtained.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08063234B2 |
| Source dataset | uspto-grants-2011_11 |
| ORD ID | ord-0bbde19fc05242369e05029fe0bb3454 |
| Source note | uspto-grants-2011_11 |