HuagongsheHuagongshe Chemistry Print Report · For research reference only
(R)-5-(5-amino-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepane-3-thione → 8-(3-((R)-6,6-difluoro-5,7,7-trimethyl-3-thioxo-1,4-oxazepan-5-yl)-4-fluorophenylamino)-5,6,7,8-tetrahydroquinoline-3-carbonitrile
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | (R)-5-(5-amino-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepane-3-thione | HCID 58563112 | — |
| Reactant | 5,6,7,8-Tetrahydro-8-oxo-3-quinolinecarbonitrile | HCID 68227243 | — |
| Product | 8-(3-((R)-6,6-difluoro-5,7,7-trimethyl-3-thioxo-1,4-oxazepan-5-yl)-4-fluorophenylamino)-5,6,7,8-tetrahydroquinoline-3-carbonitrile | HCID 86670907 | 63.2% |
Reaction Steps
Prepared in an analogous manner as described for intermediate A22A from (R)-5-(5-amino-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepane-3-thione (intermediate A19B) (102 mg, 320 μmol) and 8-oxo-5,6,7,8-tetrahydroquinoline-3-carbonitrile (66.2 mg, 384 μmol). The 8-(3-((R)-6,6-difluoro-5,7,7-trimethyl-3-thioxo-1,4-oxazepan-5-yl)-4-fluorophenylamino)-5,6,7,8-tetrahydroquinoline-3-carbonitrile (96 mg, 63.1%) was obtained as a white foam. MS (ISN): m/z=473.1 [(M−H)−].
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08748418B2 |
| Source dataset | uspto-grants-2014_06 |
| ORD ID | ord-17dd5c0153274e259247ae1490c92b5e |
| Source note | uspto-grants-2014_06 |