Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Dimethylformamide | HCID 6228 | — |
| Reactant | Cesium carbonate | HCID 10796 | — |
| Reactant | Tert-butyl 3-(methanesulfonyloxy)azetidine-1-carboxylate | HCID 10753243 | — |
| Reactant | HCID 15576447 | HCID 15576447 | — |
| Solvent | Water | HCID 962 | — |
| Product | HCID 58043101 | HCID 58043101 | 96.3% |
Reaction Steps
In a microwave vial, 4-[(4-acetylpiperazin-1-yl)methyl]phenol (1.0 g, 4.3 mmol)—see EP 50298—, tert-butyl 3-[(methylsulfonyl)oxy]azetidine-1-carboxylate (1.0 g, 4.0 mmol) and Cs2CO3 (1.5 g, 4.6 mmol) together with DMF (10 mL) was added. The mixture was heated in a microwave oven at 140° C. for 60 minutes. Water (40 mL) was added and the suspension was extracted with twice with EtOAc (50 mL). The combined organic phases were washed with brine, dried (Na2CO3) and the solvent was removed by evaporation. The residue was co-evaporated with toluene. There was obtained 1.5 g (68%) of 23A.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08546375B2 |
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| Source dataset | uspto-grants-2013_10 |
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| ORD ID | ord-7460c39fabf04c98965e433af5f6115f |
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| Source note | uspto-grants-2013_10 |
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