HuagongsheHuagongshe Chemistry Print Report · For research reference only
Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphate → N-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]-2-(2-bromophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphate | HCID 151348 | — |
| Reactant | 1-(1-Methyl-4-piperidinyl)piperazine | HCID 566324 | — |
| Reactant | N-[4-(1-methyl-4,5-dihydro-1H-imidazol-2-yl)phenyl]-2-(2-bromophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetamide | HCID 11692377 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | N-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]-2-(2-bromophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetamide | HCID 11649811 | 88.7% |
Reaction Steps
To a solution of 2-(2-bromophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetic acid (from EXAMPLE 77, 30 mg, 0.078 mmol), 1-(1-methylpiperidin-4-yl)piperazine (purchased from Oakwood products, 21 mg, 0.11 mmol) and TEA (0.0-44 mL, 0.31 mmol) in DMF (3 mL), BOP (69 mg, 0.16 mmol) was added. After being stirred at room temperature for 1 h, the mixture was concentrated in vacuo. The residue was purified by HPLC to give the titled compound as a powder (39 mg). MS 548.3 and 550.3 (M+H, Cl+Br pattern).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07678913B2 |
| Source dataset | uspto-grants-2010_03 |
| ORD ID | ord-0a3693eb3f9147488a60513d67a07c3d |
| Source note | uspto-grants-2010_03 |