HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Indole → [2-(1H-Indol-3-ylsulfanyl)benzyl]methylamine
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Indole | HCID 798 | — |
| Edukt | Trichloroacetic Acid | HCID 6421 | — |
| Edukt | Sodium Hydroxide | HCID 14798 | — |
| Edukt | 2-Methyl-2,3-dihydro-benzo[d]isothiazole | HCID 12428808 | — |
| Edukt | Ethyl acetate methanol triethylamine | HCID 21980445 | — |
| Lösungsmittel | Tetrahydrofuran | HCID 8028 | — |
| Lösungsmittel | Ethyl Acetate | HCID 8857 | — |
| Produkt | [2-(1H-Indol-3-ylsulfanyl)benzyl]methylamine | HCID 15979848 | 67% |
Reaktionsschritte
2-Methyl-2,3-dihydro-benzoisothiazole (VI) (Hoffmann, R. W.; Goldman, S. Chem. Ber. 111, 1978, 2716-2725) (75 mg, 0.50 mmol) was dissolved in THF (1 mL) and added to indole (V) (140 mg, 0.60 mmol) under Ar. Tricloroacetic acid (90 mg, 0.55 mmol) was added and the reaction mixture was stirred at room temperature for 16 hours. 2 mL 1N NaOH (aq) was added. Extraction with ethyl acetate (2×10 mL) and purification by flash chromatography on silica gel (eluent: ethyl acetate then ethyl acetate/methanol/triethylamine) gave 88 mg [2-(1H-Indol-3-ylsulfanyl)benzyl]methyl amine (67% yield).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US07737170B2 |
| Quelldatensatz | uspto-grants-2010_06 |
| ORD ID | ord-d61e73bbb6e7434bbed276ddafd1091b |
| Quellennotiz | uspto-grants-2010_06 |