HuagongsheHuagongshe Chemistry Print Report · For research reference only
Ammonium formate → 2-Amino-N-(4-methoxy-quinolin-8-yl)-4-trifluoromethyl-benzenesulfonamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Ammonium formate | HCID 2723923 | — |
| Reactant | 2-Amino-N-(7-chloro-4-methoxy-quinolin-8-yl)-4-trifluoromethyl-benzenesulfonamide | HCID 68183431 | — |
| Catalyst | Palladium | HCID 23938 | — |
| Solvent | Acetic Acid | HCID 176 | — |
| Solvent | Ethyl Acetate | HCID 8857 | — |
| Product | 2-Amino-N-(4-methoxy-quinolin-8-yl)-4-trifluoromethyl-benzenesulfonamide | HCID 68183394 | 101.3% |
Reaction Steps
10% palladium on carbon (82 mg) was added to a solution of 2-amino-N-(7-chloro-4-methoxy-quinolin-8-yl)-4-trifluoromethyl-benzenesulfonamide (Intermediate 195) (670 mg, 1.5 mmol) and ammonium formate (481 mg, 7.5 mmol) in 50% acetic acid (5 ml) and the reaction was heated under reflux for 30 min. After cooling the mixture was diluted with EtOAc (100 ml), washed sat sodium bicarbonate solution, dried (MgSO4) concentrated in vacuo. The crude residue was purified by column chromatography with DCM/MeOH (98:2) as the eluent to give the title compound (604 mg, 100%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09102688B2 |
| Source dataset | uspto-grants-2015_08 |
| ORD ID | ord-39168b1b733d4f52a2d615d0101e16f6 |
| Source note | uspto-grants-2015_08 |