Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | Bromoacetonitrile | HCID 11534 | — |
| Reactant | HCID 58246215 | HCID 58246215 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | HCID 86653002 | HCID 86653002 | — |
Reaction Steps
N-[2-({1-[1-(3-Chlorophenyl)cyclobutyl]-1,2,3,4-tetrahydroisoquinolin-7-yl}oxy)ethyl]propane-1-sulfonamide (70 mg, 0.14 mmol, cf. example 49) was dissolved in dry dichloromethane (0.5 mL). Triethylamine (35.5 mg, 0.35 mmol) was added and the reaction mixture was stirred at room temperature for 30 min. After addition of 2-bromoacetonitrile (20 mg, 0.168 mmol) stirring at room temperature was continued over night. The reaction mixture was diluted with dichloromethane and washed with aqueous saturated NaHCO3 solution (5 mL) and water (5 mL). The organic phase was dried (MgSO4) and the solvent was evaporated in vacuo. The crude product was purified by flash chromatography (silica, dichloromethane then dichloromethane:methanol=200:1). Yield: 35 mg (0.07 mmol, 50%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08653100B2 |
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| Source dataset | uspto-grants-2014_02 |
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| ORD ID | ord-7c25937baaa34390a025a4f957741f5d |
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| Source note | uspto-grants-2014_02 |
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