Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Hydrochloric Acid | HCID 313 | — |
| Reactant | Acetamide, N-(trimethylsilyl)- | HCID 25989 | — |
| Reactant | Sodium Bicarbonate | HCID 516892 | — |
| Reactant | (R)-(+)-3-Chlorostyrene oxide | HCID 10898919 | — |
| Reactant | HCID 69457148 | HCID 69457148 | — |
| Solvent | Dimethyl Sulfoxide | HCID 679 | — |
| Product | HCID 69457928 | HCID 69457928 | 59% |
Reaction Steps
To a solution of 2-{3-[(2R)-2-aminopropyl]-1H-indol-7-yl}-N,N-diethylacetamide (1.0 g, 3.48 mmol) in dimethylsulfoxide (5 mL) is added N-trimethylsilylacetamide (0.50 g, 3.83 mmol), and the mixture is stirred at room temperature for 1 hour. To the reaction solution is added (R)-(+)-3-chlorostyrene oxide (0.89 mL, 6.96 mmol), and the mixture is stirred at 110° C. for 2 hours. After cooling, a 2 N hydrochloric acid (5 mL) is added to the mixture, and the mixture is stirred at room temperature for 0.5 hour. To the mixture are added a saturated aqueous sodium hydrogen carbonate solution and a saturated brine, and the mixture is extracted with chloroform. The organic layer is dried over anhydrous sodium sulfate and concentrated. The residue is purified by silica gel column chromatography (a saturated ammonia solution in chloroform) to give the title compound (0.90 g, yield: 59%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US07217724B2 |
|---|
| Source dataset | uspto-grants-2007_05 |
|---|
| ORD ID | ord-ea1f38e574da404c9d6b98ea9e454877 |
|---|
| Source note | uspto-grants-2007_05 |
|---|