HuagongsheHuagongshe Chemistry Print Report · For research reference only
4-Aminophenyl trifluoromethyl sulphone → (2S,4S)-4-fluoro-1-[[N-[4-[N-(4-trifluoromethylsulfonylphenyl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]pyrrolidine-2-carbonitrile
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 4-Aminophenyl trifluoromethyl sulphone | HCID 136315 | — |
| Reactant | (2S,4S)-1-[[N-(4-carboxybicyclo[2,2,2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile | HCID 57634365 | — |
| Product | (2S,4S)-4-fluoro-1-[[N-[4-[N-(4-trifluoromethylsulfonylphenyl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]pyrrolidine-2-carbonitrile | HCID 57756743 | 13.2% |
Reaction Steps
In a similar manner to Example 63, (2S,4S)-1-[[N-(4-carboxybicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile (50.0 mg) and 4-trifluoromethylsulfonylaniline (77.0 mg) were used to obtain (2S,4S)-4-fluoro-1-[[N-[4-[N-(4-trifluoromethylsulfonylphenyl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]pyrrolidine-2-carbonitrile (10.8 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07560569B2 |
| Source dataset | uspto-grants-2009_07 |
| ORD ID | ord-4fa769d41de047579b6917fb55cd4b87 |
| Source note | uspto-grants-2009_07 |