HuagongsheHuagongshe Chemistry Print Report · For research reference only
3-{4-[(E)-3-(3,4-Dichloro-phenyl)-acryloyl]-7-oxo-[1,4]diazepan-1-yl}-propionic acid → 1-[(E)-3-(3,4-Dichloro-phenyl)-acryloyl]-4-[3-((3RS,4SR)-3,4-dihydroxy-piperidin-1-yl)-3-oxo-propyl]-[1,4]diazepan-5-one
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 3-{4-[(E)-3-(3,4-Dichloro-phenyl)-acryloyl]-7-oxo-[1,4]diazepan-1-yl}-propionic acid | HCID 67074538 | — |
| Reactant | (cis)-(Rac)-3,4-bis-(tert-butyl-dimethyl-silanyloxy)-piperidine | HCID 131727826 | — |
| Product | 1-[(E)-3-(3,4-Dichloro-phenyl)-acryloyl]-4-[3-((3RS,4SR)-3,4-dihydroxy-piperidin-1-yl)-3-oxo-propyl]-[1,4]diazepan-5-one | HCID 89568148 | 95% |
Reaction Steps
In analogy to the procedure described in Example 1,3-{4-[(E)-3-(3,4-dichloro-phenyl)-acryloyl]-7-oxo-[1,4]diazepan-1-yl}-propionic acid (intermediate 5) and (cis)-(rac)-3,4-bis-(tert-butyl-dimethyl-silanyloxy)-piperidine (intermediate 9) gave the titled compound in 95% yield as a white solid. MS: 712.5 (MH+, 2Cl).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08445674B2 |
| Source dataset | uspto-grants-2013_05 |
| ORD ID | ord-d806f45733a64896a09020ae61455881 |
| Source note | uspto-grants-2013_05 |