HuagongsheHuagongshe Chemistry Print Report · For research reference only
Trifluoroacetic acid → 3-[(4-Chloro-2,6-difluorophenyl)(cyclopropyl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indole
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Trifluoroacetic acid | HCID 6422 | — |
| Reactant | (4-Chloro-2,6-difluorophenyl)(cyclopropyl)methanol | HCID 58392245 | — |
| Reactant | 5-Fluoro-7-[(methylsulfonyl)methyl]-1H-indole | HCID 58392318 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | 3-[(4-Chloro-2,6-difluorophenyl)(cyclopropyl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indole | HCID 58392165 | — |
Reaction Steps
96 mg (0.44 mmol) of the compound from Example 156A 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 3 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). 162 mg (86% 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-24da6ea17b374dd4bdcfe0906fe97368 |
| Source note | uspto-grants-2011_11 |