Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Phenyl isocyanate | HCID 7672 | — |
| Reactant | HCID 15481711 | HCID 15481711 | — |
| Solvent | Acetonitrile | HCID 6342 | — |
| Solvent | Ethyl Acetate | HCID 8857 | — |
| Product | HCID 15481717 | HCID 15481717 | 84.6% |
Reaction Steps
To a ice cooled solution of (2R,3R)-2-(2,4-diflurophenyl)-3-(piperazin-1-yl)-1-(1H-1,2,4-triazole-1-yl)butan-2-ol 2 (150 mg, 0.44 mmol) in acetonitrile (10 ml) was added phenylisocyanate (60 mg, 0.5 mmol) in acetonitrile (4 ml). The reaction mixture was stirred at 0° C. for 2 h, diluted with 20 ml of ethyl acetate and successively washed with water, brine and dried over sodium sulphate. This organic extract was concentrated and the residue was purified by passing through a column of silica gel (hexane/EtOAc) to give the title compound as a colorless solid (170 mg, 84%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US06153616 |
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| Source dataset | uspto-grants-2000_11 |
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| ORD ID | ord-9a92e15ce71745b39b0c1a553c663853 |
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| Source note | uspto-grants-2000_11 |
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