HuagongsheHuagongshe Chemistry Print Report · For research reference only
1,2-Dichloroethane → N-[[2-(3-Chlorophenyl)-5-(trifluoromethyl)-2H-pyrazol-3-yl]-methyl]-2-[4-[[(ethylsulfonyl)amino]-methyl]-3-fluoro-phenyl]-propionamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 1,2-Dichloroethane | HCID 11 | — |
| Reactant | 1-Hydroxybenzotriazole | HCID 75771 | — |
| Reactant | (1-(3-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl)methanamine | HCID 66644230 | — |
| Reactant | 2-(4-(Ethylsulfonamidomethyl)-3-fluorophenyl)propanoic acid | HCID 70816569 | — |
| Solvent | 1,4-Dioxane | HCID 31275 | — |
| Product | N-[[2-(3-Chlorophenyl)-5-(trifluoromethyl)-2H-pyrazol-3-yl]-methyl]-2-[4-[[(ethylsulfonyl)amino]-methyl]-3-fluoro-phenyl]-propionamide | HCID 70816450 | — |
Reaction Steps
2-(4-(ethyl-sulfonamidomethyl)-3-fluorophenyl)propanoic acid (60 mg, 0.207 mmol) and (1-(3-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl)methanamine (63 mg, 0.228 mmol) were dissolved and mixed in 1,4-dioxane followed by addition of HOBt (42 mg, 0.310 mmol) and EDC (60 mg, 0.313 mmol) and TEA (0.07 mL, 0.518 mmol). The reaction mixture was stirred for overnight and then quenched by water and extracted with EtOAc. Drying (MgSO4) and evaporation of the ethyl acetate followed and the residue was purified by CC (EtOAc/n-hexane) to give the example B17 in pure form (104 mg, 92%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08946204B2 |
| Source dataset | uspto-grants-2015_02 |
| ORD ID | ord-f5165c45d53541fcabadbf8c95729c4f |
| Source note | uspto-grants-2015_02 |