HuagongsheHuagongshe Chemistry Print Report · For research reference only
Triethylamine → 6-oxo-N-[3-(1-trityl-1H-imidazol-4-yl)phenyl]-7,8,9,10-tetrahydro-6H-pyrido[3',2':4,5]pyrrolo[1,2-a][1,4]diazepine-2-carboxamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | PyBOP | HCID 2724699 | — |
| Reactant | 3-(1-trityl-1H-imidazol-4-yl)aniline | HCID 11475113 | — |
| Reactant | 6-Oxo-7,8,9,10-tetrahydro-6H-pyrido[3',2':4,5]pyrrolo[1,2-a][1,4]diazepine-2-carboxylic acid | HCID 67236342 | — |
| Solvent | Water | HCID 962 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | 6-oxo-N-[3-(1-trityl-1H-imidazol-4-yl)phenyl]-7,8,9,10-tetrahydro-6H-pyrido[3',2':4,5]pyrrolo[1,2-a][1,4]diazepine-2-carboxamide | HCID 67237224 | 68.4% |
Reaction Steps
A solution of 6-Oxo-7,8,9,10-tetrahydro-6H-pyrido[3′,2′:4,5]pyrrolo[1,2-a][1,4]diazepine-2-carboxylic acid (Intermediate E, 50 mg, 0.20 mmol) and PyBOP (159 mg, 0.31 mmol) in DMF (1.5 mL) is stirred for 30 min. 3-(1-Trityl-1H-imidazol-4-yl)-phenylamine (86 mg, 0.21 mmol) and triethylamine (57 μL, 0.41 mmol) are added and the reaction is stirred at room temperature for 16 h. The mixture is poured into H2O and the resulting white solid is collected by filtration and dried in vacuo to afford the title compound (86 mg, 67%) which was used in the next step without further purification.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09073926B2 |
| Source dataset | uspto-grants-2015_07 |
| ORD ID | ord-606a6a58863043b59045d53f1f6b96a0 |
| Source note | uspto-grants-2015_07 |