Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Piperazine | HCID 4837 | — |
| Reactant | Triphenylphosphine | HCID 11776 | — |
| Reactant | Diisopropyl azodicarboxylate | HCID 5363146 | — |
| Reactant | HCID 178518547 | HCID 178518547 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | HCID 178518546 | HCID 178518546 | 47.7% |
Reaction Steps
To a solution of 2-{[(4-{[4-chloro-3-(trifluoromethyl)phenyl]oxy}phenyl)methyl]thio}-5-(hydroxymethyl)-4(1H)-pyrimidinone (51 mg, 0.115 mmol) in dry DMF (3 mL) was added DIAD (0.034 mL, 0.173 mmol), triphenylphosphine (45.3 mg, 0.173 mmol) and piperizine (19.61 mg, 0.230 mmol) under argon. The mixture was heated with a microwave reactor at 45° C. for 0.5 h. Purification via MDAP then afforded the title compound (28 mg, 47.7% yield). LCMS: rt=3.02 min, [M+H+]=510
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08637536B2 |
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| Source dataset | uspto-grants-2014_01 |
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| ORD ID | ord-38228156f6914af292d9f831f8ece132 |
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| Source note | uspto-grants-2014_01 |
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