HuagongsheHuagongshe Chemistry Print Report · For research reference only
5-Chloro-2-(trifluoromethyl)phenylboronic acid → Ethyl 2-{4-[5-chloro-2-(trifluoromethyl)phenyl]-2-oxopyridin-1(2H)-yl}-3-cyclopropylpropanoate
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 5-Chloro-2-(trifluoromethyl)phenylboronic acid | HCID 46736817 | — |
| Reactant | Ethyl 2-(4-bromo-2-oxopyridin-1(2H)-yl)-3-cyclopropylpropanoate | HCID 117622870 | — |
| Catalyst | HCID 178418397 | HCID 178418397 | — |
| Product | Ethyl 2-{4-[5-chloro-2-(trifluoromethyl)phenyl]-2-oxopyridin-1(2H)-yl}-3-cyclopropylpropanoate | HCID 117622749 | — |
Reaction Steps
250 mg (0.8 mmol) of ethyl 2-(4-bromo-2-oxopyridin-1(2H)-yl)-3-cyclopropylpropanoate (racemate) and 214 mg (0.96 mmol) of 5-chloro-2-trifluoromethylphenylboronic acid in the presence of tetrakis(triphenylphosphine)palladium(0) were reacted according to General Method 2A. Yield: 35 mg (purity 87%, 9% of theory) of the title compound and 70 mg (22% of theory) of the product which is already hydrolysed (Example 6.1F)
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09434690B2 |
| Source dataset | uspto-grants-2016_09 |
| ORD ID | ord-6a2cf857d0c7401f9a68c29b8c5a1197 |
| Source note | uspto-grants-2016_09 |