HuagongsheHuagongshe Chemistry Print Report · For research reference only
N-methyl-2-pyrrolidone → 3-(6-tert-Butyl-4-trifluoromethyl-pyridin-3-yl)-N-(3-ethynyl-5-fluoro-4-methanesulfonylamino-benzyl)-acrylamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | N-methyl-2-pyrrolidone | HCID 13387 | — |
| Reactant | 3-(6-Tert-butyl-4-trifluoromethyl-pyridin-3-yl)-acrylic acid | HCID 68784901 | — |
| Reactant | 3-Ethynyl-5-fluoro-4-methansulfonylaminobenzylamine hydrochloride | HCID 86625519 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | 3-(6-tert-Butyl-4-trifluoromethyl-pyridin-3-yl)-N-(3-ethynyl-5-fluoro-4-methanesulfonylamino-benzyl)-acrylamide | HCID 74332388 | 30.2% |
Reaction Steps
N-(4-Aminomethyl-2-ethynyl-6-fluoro-phenyl)-methanesulfonamide HCl salt (11.2 mg, 0.04 mmol) was reacted with 3-(6-tert-butyl-4-trifluoromethyl-pyridin-3-yl)-acrylic acid (1.0 eq, 11.0 mg) DMTMM (1.0 eq, 11.1 mg) and NMP (1.2 eq, 6 μl) in THF to give the title compound (6 mg, 30.2%) after purification by column chromatography (Hex/EtOAc=3/2).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07858621B2 |
| Source dataset | uspto-grants-2010_12 |
| ORD ID | ord-223f31e459144b88a91c51f9a718f432 |
| Source note | uspto-grants-2010_12 |