HuagongsheHuagongshe Chemistry Print Report · For research reference only
4-Amino-3-(trifluoromethyl)benzoic acid → 2-(1-{[4-Amino-3-(trifluoromethyl)phenyl]carbonyl}piperidin-4-yl)-5-(3,4-dimethoxyphenyl)-4,4-dimethyl-2,4-dihydro-3H-pyrazol-3-one
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 4-Amino-3-(trifluoromethyl)benzoic acid | HCID 3254286 | — |
| Reactant | 5-(3,4-dimethoxyphenyl)-4,4-dimethyl-2-piperidin-4-yl-2,4-dihydro-3H-pyrazol-3-one hydrochloride | HCID 66616406 | — |
| Product | 2-(1-{[4-Amino-3-(trifluoromethyl)phenyl]carbonyl}piperidin-4-yl)-5-(3,4-dimethoxyphenyl)-4,4-dimethyl-2,4-dihydro-3H-pyrazol-3-one | HCID 46206626 | — |
Reaction Steps
The title compound is prepared analogously as described for GP3 using 5-(3,4-dimethoxyphenyl)-4,4-dimethyl-2-(piperidin-4-yl)-2,4-dihydro-3H-pyrazol-3-one (compound B1) and 4-amino-3-(trifluoromethyl)benzoic acid as starting compounds. The crude product is purified by column chromatography (silica gel and DCM/methanol=4:1) and crystallization from methanol to yield the title compound.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08609848B2 |
| Source dataset | uspto-grants-2013_12 |
| ORD ID | ord-cf51dd9c9a57448b9b9e0ff39c9eed23 |
| Source note | uspto-grants-2013_12 |