Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Water | HCID 962 | — |
| Reactant | Sodium hydride | HCID 24758 | — |
| Reactant | 2-(4-Chlorophenyl)-2-methyloxirane | HCID 160587 | — |
| Reactant | 9-Chloro-3-methyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indole | HCID 68558507 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | HCID 59368218 | HCID 59368218 | 43.6% |
Reaction Steps
The title compound was prepared by following general procedure 5. To a stirred suspension of sodium hydride (61 mg, 0.254 mmol) in 5 mL of DMF, 9-chloro-3-methyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indole (0.2 g, 0.852 mmol) was added and stirred at RT for 5 min. 2-(4-Chlorophenyl)-2-methyloxirane (214 mg, 1.27 mmol) was added slowly dropwise and stirred at RT for 14 h. The reaction was monitored by TLC and LCMS. After completion of the reaction, water was added, extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate, evaporated under reduced pressure and purified by reverse phase chromatography to afford 150 mg of (1-(9-chloro-3-methyl-2,3,4,5-tetrahydroazepino[4,5-b]indol-6(1H)-yl)-2-(4-chlorophenyl)propan-2-ol) as the TFA salt.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08569287B2 |
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| Source dataset | uspto-grants-2013_10 |
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| ORD ID | ord-93f7de55d27c4ac8a1e5fc2413851eef |
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| Source note | uspto-grants-2013_10 |
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