Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Methyl iodide | HCID 6328 | — |
| Reactant | Sodium hydride | HCID 24758 | — |
| Reactant | HCID 57074082 | HCID 57074082 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Solvent | Sodium chloride; water | HCID 57417360 | — |
| Product | HCID 57006595 | HCID 57006595 | 23.2% |
Reaction Steps
To a solution of (2R)-1-[3,5-bis(trifluoromethyl)-benzoyl]-2-[4-methyl-3-(trifluoroacetylamino)benzyl]-4-[2-[(2S)-2-(methoxymethyl)morpholino]ethyl]piperazine (131 mg) in tetrahydrofuran (2 ml) was added sodium hydride (10 mg) and the resulting mixture was stirred for 20 minutes. Methyl iodide (28 mg) was added to the mixture and the whole was stirred at room temperature overnight. Brine was added to the mixture and the organic layer was separated, dried over magnesium sulfate, and evaporated in vacuo. The residue was purified by HPLC to give (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-[4-methyl-3-(N-methyl-N-trifluoroacetylamino)benzyl]-4-[2-[(2S)-2-(methoxymethyl)-morpholino]ethyl]piperazine (31 mg) as an oil. The obtained compound was converted to its dihydrochloride in a conventional manner.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US07166598B2 |
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| Source dataset | uspto-grants-2007_01 |
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| ORD ID | ord-ed6a5ece6c2f4b69aeb35eab66402aa5 |
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| Source note | uspto-grants-2007_01 |
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