HuagongsheHuagongshe Chemistry Print Report · For research reference only
1-Hydroxybenzotriazole → Methyl cis(+/-)-3-(4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)benzoate
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 1-Hydroxybenzotriazole | HCID 75771 | — |
| Reactant | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| Reactant | 4-chloro-5-ethyl-1H-imidazole-2-carboxylic acid | HCID 67548929 | — |
| Reactant | Methyl cis(+/-)-3-(4-amino-3-methoxypiperidin-1-yl)benzoate | HCID 86648708 | — |
| Product | Methyl cis(+/-)-3-(4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)benzoate | HCID 86648707 | — |
Reaction Steps
The same operation as in Example (1g) was performed using methyl cis(±)-3-(4-amino-3-methoxypiperidin-1-yl)benzoate obtained in Example (164a) (116.41 mg, 0.44 mmol), 4-chloro-5-ethyl-1H-imidazole-2-carboxylic acid obtained by the method described in Example (1d) (73 mg, 0.42 mmol), WSC hydrochloride (241.23 mg, 1.26 mmol) and HOBt (56.72 mg, 0.42 mmol), to obtain 148.3 mg of the title compound as a pale yellow oily substance (81%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08536197B2 |
| Source dataset | uspto-grants-2013_09 |
| ORD ID | ord-a1f27b49bef442d9a07543f071342219 |
| Source note | uspto-grants-2013_09 |