HuagongsheHuagongshe Chemistry Print Report · For research reference only
Cesium carbonate → N-Cyclopropylmethyl-4-(4,6-dimethoxy-pyrimidin-2-ylamino)-2-trifluoromethyl-benzenesulfonamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Cesium carbonate | HCID 10796 | — |
| Reactant | 2-Amino-4,6-dimethoxypyrimidine | HCID 118946 | — |
| Reactant | Binap, (A+-)- | HCID 634876 | — |
| Reactant | 4-bromo-N-(cyclopropylmethyl)-2-(trifluoromethyl)benzenesulfonamide | HCID 24948367 | — |
| Catalyst | palladium(II) acetate | HCID 167845 | — |
| Solvent | Toluene | HCID 1140 | — |
| Product | N-Cyclopropylmethyl-4-(4,6-dimethoxy-pyrimidin-2-ylamino)-2-trifluoromethyl-benzenesulfonamide | HCID 24948181 | 41% |
Reaction Steps
Mixture of 4-bromo-N-cyclopropylmethyl-2-trifluoromethylbenzenesulfonamide (228 mg, 0.63 mmol), 2,-amino-4,6-dimethoxypyrimidine (156 mg, 1.0 mmol), Pd(OAc)2 (26 mg, 0.11 mmol), BINAP (78 mg, 0.12 mmol) and cesium carbonate (362 mg, 1.11 mmol) in 15 ml toluene was relaxed for 6 hours. Toluene was evaporated in vacuum and crude oil was purified by Combiflash (PE-THF). Yield 41%
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09422235B2 |
| Source dataset | uspto-grants-2016_08 |
| ORD ID | ord-c1285f582f9843faa8af9afb7e28de0e |
| Source note | uspto-grants-2016_08 |