HuagongsheHuagongshe Chemistry Print Report · For research reference only
N-methyl-2-pyrrolidone → 3-(2-Bromo-6-tert-butyl-pyridin-3-yl)-N-(3-fluoro-4-methane sulfonylamino-benzyl)-acrylamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | N-methyl-2-pyrrolidone | HCID 13387 | — |
| Reactant | N-[4-(aminomethyl)-2-fluorophenyl]methanesulfonamide hydrochloride | HCID 21097525 | — |
| Reactant | 3-(2-Bromo-6-tert-butyl-pyridin-3-yl)-acrylic acid | HCID 86625523 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | 3-(2-Bromo-6-tert-butyl-pyridin-3-yl)-N-(3-fluoro-4-methane sulfonylamino-benzyl)-acrylamide | HCID 74332390 | 32.8% |
Reaction Steps
3-Fluoro-4-methanesulfonylaminobenzylamine hydrochloride (116 mg, 0.454 mmol) was reacted with 3-(2-bromo-6-tert-butyl-pyridin-3-yl)-acrylic acid (1.0 eq, 129 mg) DMTMM (1.0 eq, 126 mg) and NMP (1.2 eq, 60 μl) in THF to give the title compound (72 mg, 32.8%) after purification by column chromatography (Hex/EtOAc=1/1).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07858621B2 |
| Source dataset | uspto-grants-2010_12 |
| ORD ID | ord-94a052e39cb94f4cbd96a6ec4ecfdd3b |
| Source note | uspto-grants-2010_12 |