Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Sulfamide | HCID 82267 | — |
| Reactant | HCID 178444599 | HCID 178444599 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | HCID 59249272 | HCID 59249272 | — |
Reaction Steps
To a stirred solution of rac-4-{[(2R,3S,4R,5S)-3-(3-Chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-trans-cyclohexylamine trifluoroacetic acid salt (50 mg, 0.091 mmol) in THF (3 mL), sulfamide (Aldrich, 40 mg, 0.416 mmol) was added and the mixture was stirred at 110° C. for 25 min. on microwave oven. The reaction was quenched with addition of water. The mixture was extracted with EtOAc (2×10 mL) and the extracts were dried with magnesium sulfate. The solvent was removed and the residue was purified on a reverse phase HPLC (25-90, acetonitrile/water) to give a white solid. 49 mg.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US08354444B2 |
|---|
| Source dataset | uspto-grants-2013_01 |
|---|
| ORD ID | ord-cfc694e8a96c4edaa2ea4ddbb9d1afc6 |
|---|
| Source note | uspto-grants-2013_01 |
|---|