HuagongsheHuagongshe Chemistry Print Report · For research reference only
3-Chloro-4-fluorophenylboronic Acid (contains varying amounts of Anhydride) → 4-Hydroxy-4'-trifluoromethyl-biphenyl-3-carboxylic acid [2-(3'-chloro-4'-fluoro-6-methoxy-biphenyl-3-yl)-ethyl]-amide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 3-Chloro-4-fluorophenylboronic Acid (contains varying amounts of Anhydride) | HCID 2734660 | — |
| Reactant | 2-(3-Bromo-4-methoxyphenyl)ethan-1-amine | HCID 2735581 | — |
| Reactant | 2-hydroxy-5-[4-(trifluoromethyl)phenyl]benzoic Acid | HCID 2782701 | — |
| Product | 4-Hydroxy-4'-trifluoromethyl-biphenyl-3-carboxylic acid [2-(3'-chloro-4'-fluoro-6-methoxy-biphenyl-3-yl)-ethyl]-amide | HCID 11249750 | 24.5% |
Reaction Steps
The resin-bound 4-hydroxy-4′-trifluoromethyl-biphenyl-3-carboxylic acid (20 mg, 0.06 mmol) obtained as in Example 1 was reacted with 3-bromo-4-methoxy-phenethyl amine (57 mg, 0.25 mmol) following general procedure A to give resin bound 4-Hydroxy-4′-trifluoromethyl-biphenyl-3-carboxylic acid [2-3-bromo-4-methoxy-phenyl)-ethyl]-amide(18 mg, 0.05 mmol). The above resin bound amide was treated with 3-chloro-4-fluoro-phenyl boronic acid (43 mg, 0.25 mmol) as described in the general procedure D to provide the title compound (8.0 mg,).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07459472B2 |
| Source dataset | uspto-grants-2008_12 |
| ORD ID | ord-4c7e4a753f2a40db88c296372a7c3f7b |
| Source note | uspto-grants-2008_12 |