HuagongsheHuagongshe Chemistry Print Report · For research reference only
Trifluoroacetic acid → N-cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-5-{[(1H-imidazol-2-ylmethyl)amino]methyl}-1H-1,2,3-triazole-4-carboxamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Trifluoroacetic acid | HCID 6422 | — |
| Reactant | N-cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-5-({[(1-trityl-1H-imidazol-2-yl)methyl]amino}methyl)-1H-1,2,3-triazole-4-carboxamide | HCID 57664825 | — |
| Product | N-cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-5-{[(1H-imidazol-2-ylmethyl)amino]methyl}-1H-1,2,3-triazole-4-carboxamide | HCID 57664919 | 61.2% |
Reaction Steps
Trifluoroacetic acid (0.5 ml) was added to N-cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-5-({[(1-trityl-1H-imidazol-2-yl)methyl]amino}methyl)-1H-1,2,3-triazole-4-carboxamide (78 mg, 0.12 mmol) obtained in Example 1198, and the mixture was stirred at room temperature for 1 hr. The reaction mixture was concentrated, water (2 ml) was added to the residue, and precipitated crystals were filtered off. The filtrate was neutralized with 1N aqueous sodium hydroxide solution and concentrated to dryness. The residue was purified by silica gel column (hexane/ethyl acetate=1/1 to ethyl acetate/methanol=4/1) to give the title compound as a colorless powder (30 mg, 61%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07803822B2 |
| Source dataset | uspto-grants-2010_09 |
| ORD ID | ord-b7c1657b78c64a5089ae742c45f6b93f |
| Source note | uspto-grants-2010_09 |