Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Water | HCID 962 | — |
| Reactant | 4-Aminopyridine | HCID 1727 | — |
| Reactant | 1,1'-Carbonyldiimidazole | HCID 68263 | — |
| Reactant | 3-[6-fluoro-3-(4-fluorobenzyl)-3,4-dihydroisoquinolin-2(1H)-yl]propanamine | HCID 59323293 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | HCID 59323453 | HCID 59323453 | 12.1% |
Reaction Steps
60 mg of 3-[6-fluoro-3-(4-fluorobenzyl)-3,4-dihydroisoquinolin-2(1H)-yl]propanamine obtained in Example 238-b), 20 mg of 4-aminopyridine, and 34 mg of CDI were dissolved in 1.2 mL of THF, followed by stirring at 60° C. for 3 hours. After completion of the reaction, water was added to the reaction liquid, followed by extraction with chloroform. The organic layer was then washed with saturated brine, dried over anhydrous sodium sulfate and then concentrated under reduced pressure. The residue obtained was purified using silica gel chromatography (chloroform:methanol=10:1) to obtain 10 mg (yield 12%) of a title compound as a yellow oily substance.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08273766B2 |
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| Source dataset | uspto-grants-2012_09 |
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| ORD ID | ord-3549afca0b9e4fe288c76ddf76e9a1f4 |
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| Source note | uspto-grants-2012_09 |
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