HuagongsheHuagongshe Chemistry Print Report · For research reference only
Triethylamine → 1-{[5-(2-Bromo-5-chlorophenyl)-1,2,4-oxadiazol-3-yl]methyl}-2-propyl-4-(trifluoromethyl)-1H-indole-5-carbonitrile
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | 2-Bromo-5-chlorobenzoyl chloride | HCID 20535425 | — |
| Reactant | HCID 178438386 | HCID 178438386 | — |
| Solvent | Acetonitrile | HCID 6342 | — |
| Product | 1-{[5-(2-Bromo-5-chlorophenyl)-1,2,4-oxadiazol-3-yl]methyl}-2-propyl-4-(trifluoromethyl)-1H-indole-5-carbonitrile | HCID 57800369 | 36% |
Reaction Conditions
| Temperature | 150 °C |
|---|
Reaction Steps
To a solution of 2-[5-cyano-2-propyl-4-(trifluoromethyl)-1H-indol-1-yl]-N-hydroxyethanimidamide (Example 275A) (0.05 g, 0.154 mmol) in anhydrous acetonitrile (10.0 mL) under N2, was added 2-bromo-5-chlorobenzoyl chloride (0.134 g, 0.529 mmol) and triethylamine (1.0 mL, 13.6 mmol). The mixture was then heated in a microwave at 150° C. for 30 min. Upon cooling, the mixture was poured onto a biotage prepak column and the mixture was purified by flash chromatography (0-25% EtOAc-hexanes gradient) to give 0.029 g (36% yield) of pure product: MS (ES) m/z 523 (M+1).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07572820B2 |
| Source dataset | uspto-grants-2009_08 |
| ORD ID | ord-7b18b5fbcc7047068f07d6f370217f43 |
| Source note | uspto-grants-2009_08 |