Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Pyridine | HCID 1049 | — |
| Reactant | Chloroacetyl chloride | HCID 6577 | — |
| Reactant | 7-amino-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one | HCID 23156738 | — |
| Solvent | Benzene | HCID 241 | — |
| Product | HCID 57558094 | HCID 57558094 | 56% |
Reaction Steps
The 7-amino-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one (100 mg, 0.329 mmol) obtained in step C of Example 1-1 was dissolved in benzene (2 ml). Thereafter, chloroacetic acid chloride (29 μl, 0.362 mmol) and pyridine (80 μl, 0.986 mmol) were added to the solution, and the obtained mixture was stirred at a room temperature for 4 hours. Thereafter, the reaction solution was washed with 1 N hydrochloric acid, and was then extracted with ethyl acetate. The extract was dried over anhydrous sodium sulfate. The solvent was distilled away under reduced pressure. The obtained residue was suspended in and washed with cold ethyl acetate, and a solid was collected by filtration, so as to obtain 2-chloro-N-[1-oxo-3-(2-trifluoromethylphenyl)-1,2-dihydroisoquinolin-7-yl]acetamide (70 mg, 56%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US07820693B2 |
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| Source dataset | uspto-grants-2010_10 |
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| ORD ID | ord-1741c9ba40fa409ead71c96dcc25356c |
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| Source note | uspto-grants-2010_10 |
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