Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Methanol | HCID 887 | — |
| Reactant | Potassium Carbonate | HCID 11430 | — |
| Reactant | Tosylmethyl isocyanide | HCID 161915 | — |
| Reactant | 5-Fluoro-1H-indole-2-carbaldehyde | HCID 18968129 | — |
| Solvent | Hexane | HCID 8058 | — |
| Product | HCID 71060591 | HCID 71060591 | 72% |
Reaction Steps
To a 100 mL round-bottom flask was added 5-fluoro-1H-indole-2-carbaldehyde 47 (0.627 g, 3.84 mmol), methanol (40 mL), p-toluene sulfonylmethyl isocyanide (0.826 g, 4.23 mmol), followed by potassium carbonate (0.68 g, 4.92 mmol). The reaction mixture was stirred at reflux for about 1.5 hour and followed by TLC. The solvent was then evaporated and saturated aq. NaHCO3 was added. The resultant suspension was extracted with CH2Cl2 (2×20 mL). Combined organic layers were washed with brine, dried (anhydrous Na2SO4), and concentrated to leave a yellow solid. Crude product was further purified by silica-column chromatographed (Biotage) using Acetone:Hexane as an eluent to yield 5-(5-fluoro-1H-indol-2-yl)oxazole 48 (0.202 g, 72% yield). MS (ES) m/z 203 (M+H+).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08865709B2 |
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| Source dataset | uspto-grants-2014_10 |
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| ORD ID | ord-9f8c221e1afd459aa6da7ce0256a3845 |
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| Source note | uspto-grants-2014_10 |
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