HuagongsheHuagongshe Chemistry Print Report · For research reference only
4-Methylmorpholine → N-[(5-fluoro-1-methyl-indole-2-cabonyl)valinyl]-3-amino-4-hydroxy-5-(2,3,5,6-tetrafluorophenyloxy)-pentanoic Acid, tert-butyl Ester
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 4-Methylmorpholine | HCID 7972 | — |
| Reactant | 1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide | HCID 15908 | — |
| Reactant | 1-Hydroxybenzotriazole | HCID 75771 | — |
| Reactant | 5-Fluoro-1-methyl-1H-indole-2-carboxylic acid | HCID 662546 | — |
| Reactant | valinyl-3-amino-4-hydroxy-5-(2,3,5,6-tetrafluorophenyloxy)-pentanoic Acid, tert-butyl Ester | HCID 131723667 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | N-[(5-fluoro-1-methyl-indole-2-cabonyl)valinyl]-3-amino-4-hydroxy-5-(2,3,5,6-tetrafluorophenyloxy)-pentanoic Acid, tert-butyl Ester | HCID 86756374 | — |
Reaction Steps
The procedure of Example 77 was followed using the product of Example 106 (212.5 mg, 0.47 mmol), 5-fluoro-1-methylindole-2-carboxylic acid (181 mg, 0.94 mmol ), NMM (0.05 ml, 0.44 mmol), HOBt (151 mg, 1.03 mmol), and EDAC (196 mg, 1.03 mmol) in methylene chloride to prepare the title product.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US06489353B2 |
| Source dataset | uspto-grants-2002_12 |
| ORD ID | ord-8d1ec93078d84df3b71d268580cfc659 |
| Source note | uspto-grants-2002_12 |