HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 448577Generated: October 29, 2026
N-Fluorobenzenesulfonimide → 4-[5-Fluoro-6-(5-methanesulfonyl-2,3-dihydro-indol-1-yl)-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid tert-butyl ester
https://huagongshe.com/reaction/448577
Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | N-Fluorobenzenesulfonimide | HCID 588007 | — |
| Reactant | Tert-butyl 4-((6-(5-(methylsulfonyl)indolin-1-yl)pyrimidin-4-yl)oxy)piperidine-1-carboxylate | HCID 25242414 | — |
| Solvent | 1,2-Dichloroethane | HCID 11 | — |
| Product | 4-[5-Fluoro-6-(5-methanesulfonyl-2,3-dihydro-indol-1-yl)-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid tert-butyl ester | HCID 58116601 | — |
Reaction Steps
4a (43 mg, 0.09 mmol) was dissolved in 1 mL of DCE with N-fluorobenzenesulfonimide (62 mg, 0.2 mmol). The mixture was stirred for 2 days at 75° C. then the solvent was evaporated under vacuum. The crude material was dissolved in 20% of DCM in methanol and purified by preparative HPLC to give 13-1; LCMS 493.1 (MH+), tR=5.21 (Method 5). EC50: 382 nM.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08481731B2 |
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| Source dataset | uspto-grants-2013_07 |
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| ORD ID | ord-d2ad9ba67206444c98b729700748fb95 |
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| Source note | uspto-grants-2013_07 |
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