HuagongsheHuagongshe Chemistry Print Report · For research reference only
Triethylamine → HCID 57917582, compound
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | 4-Amino-3-fluorobenzoic acid | HCID 9971 | — |
| Reactant | Propylphosphonic anhydride | HCID 111923 | — |
| Reactant | HCID 57917674 | HCID 57917674 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | HCID 57917582 | HCID 57917582 | 74.4% |
Reaction Steps
1-Propanephosphonic acid cyclic anhydride (1.967 g, 3 mmol, 1.840 mL, 50% solution in ethyl acetate) was added dropwise to a solution of (R)N-tert-butyl-3-((2-methylpiperazin-1-yl)methyl)benzamide (500 mg, 1.7 mmol), 4-amino-3-fluorobenzoic acid (239.7 mg, 1.5 mmol) and triethylamine (469 mg, 4.5 mmol, 1.84 mL) in dichloromethane. The reaction was stirred at room temperature for 2 hours. The dichloromethane was removed under reduced pressure and the residue was taken up in ethyl acetate, washed with water, sodium hydrogen carbonate and brine. The organic layer was concentrated under vacuum to afford the title compound (476.3 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08314091B2 |
| Source dataset | uspto-grants-2012_11 |
| ORD ID | ord-c47a4f4b93fe4c72b12dd032d618dd2f |
| Source note | uspto-grants-2012_11 |