HuagongsheHuagongshe Chemistry Print Report · For research reference only
8-Aminoquinoline → 1-(Quinolin-8-ylamino)-4-(5-fluoro-2-methoxyphenyl)-4-methyl-2-(trifluoromethyl)pentan-2-ol
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 8-Aminoquinoline | HCID 11359 | — |
| Reactant | 2-[2-(5-Fluoro-2-methoxyphenyl)-2-methylpropyl]-2-trifluoromethyloxirane | HCID 16099239 | — |
| Solvent | 2(1H)-Pyrimidinone, tetrahydro- | HCID 74615 | — |
| Product | 1-(Quinolin-8-ylamino)-4-(5-fluoro-2-methoxyphenyl)-4-methyl-2-(trifluoromethyl)pentan-2-ol | HCID 21948861 | 77.5% |
Reaction Steps
200 mg (0.68 mmol) of 2-[2-(5-fluoro-2-methoxyphenyl)-2-methylpropyl)-2-(trifluoromethyl)oxirane (WO 00/32584) and 99 mg (0.68 mmol) of 8-aminoquinoline are heated in 0.2 ml of 3,4,5,6-tetrahydro-2-(1H)-pyrimidone (DMPU) for 20 hours to 130° C. After the reaction mixture is purified on silica gel with hexane-ethyl acetate (0-20%), 230 mg of the product is obtained.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US06897224B2 |
| Source dataset | uspto-grants-2005_05 |
| ORD ID | ord-ebcaf543ef084a0e9657b4732b0f978d |
| Source note | uspto-grants-2005_05 |