HuagongsheHuagongshe Chemistry Print Report · For research reference only
1-Hydroxybenzotriazole → tert-Butyl cis(+/-)-4-{[(5-ethyl-4-iodo-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-carboxylate
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 1-Hydroxybenzotriazole | HCID 75771 | — |
| Reactant | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| Reactant | (3R,4S)-4-Amino-1-boc-3-methoxypiperidine | HCID 57362389 | — |
| Reactant | 5-ethyl-4-iodo-1H-imidazole-2-carboxylic acid | HCID 67548838 | — |
| Product | tert-Butyl cis(+/-)-4-{[(5-ethyl-4-iodo-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-carboxylate | HCID 86648514 | 86% |
Reaction Steps
The same operation as in Example (1g) was performed using tert-butyl cis(±)-4-amino-3-methoxypiperidine-1-carboxylate obtained by the method described in Example (1e) (130 mg, 0.56 mmol), 5-ethyl-4-iodo-1H-imidazole-2-carboxylic acid obtained in Example (58b) (95 mg, 0.36 mmol), WSC hydrochloride (220 mg, 1.15 mmol) and HOBT (46 mg, 0.34 mmol), to obtain 146.2 mg of the title compound as a white solid (86%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08927588B2 |
| Source dataset | uspto-grants-2015_01 |
| ORD ID | ord-4600ac6136bc4dccbdfc890fd3fe2ec9 |
| Source note | uspto-grants-2015_01 |