Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | Methyl vinyl sulfone | HCID 19354 | — |
| Reactant | 6-fluoro-1-(phenylsulfonyl)-3-(1H-pyrazol-4-yl)-1H-indole | HCID 118060134 | — |
| Solvent | Methanol | HCID 887 | — |
| Product | HCID 118060759 | HCID 118060759 | 58% |
Reaction Steps
A mixture of 6-fluoro-1-(phenylsulfonyl)-3-(1H-pyrazol-4-yl)-1H-indole (Intermediate 5; 210 mg; 0.62 mmol), methyl vinyl sulfone (654 mg; 6.16 mmol) and Et3N (0.26 mL; 1.85 mmol) in methanol (15 mL) was heated at 130° C. for 0.5 h in a microwave reactor. The reaction mixture was cooled to r.t., concentrated to give a residue which was triturated with MeOH (2 mL) to afford 160 mg (58%) of the title product as a white solid.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US09126984B2 |
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| Source dataset | uspto-grants-2015_09 |
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| ORD ID | ord-02b8675b3e3d4503b53d1191e3c1429e |
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| Source note | uspto-grants-2015_09 |
|---|