HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
4-Methylmorpholine → 3-fluoro-N-[3-(7-pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenyl]-benzenesulfonamide
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | 4-Methylmorpholine | HCID 7972 | — |
| Edukt | 3-Fluorobenzenesulfonyl Chloride | HCID 2734258 | — |
| Edukt | 3-(7-Pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenylamine | HCID 46929183 | — |
| Lösungsmittel | Dichloromethane | HCID 6344 | — |
| Produkt | 3-fluoro-N-[3-(7-pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenyl]-benzenesulfonamide | HCID 58477090 | 58,5% |
Reaktionsschritte
3-(7-Pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenylamine (prepared as described in Example 1) (30 mg, 0.102 mmol) was dissolved in dry DCM (1 mL). At room temperature 3-fluorobenzensulfonylchloride (0.014 mL, 0.107 mmol, 1.05 eq) was added followed by NMM (0.012 mL, 0.107 mmol, 1.05 eq) and the mixture was stirred for 1 hour. It was then diluted with DCM and washed with water and brine. The organic layer was dried over Na2SO4 and concentrated under reduced pressure. The crude product was purified by chromatography on silica gel (eluant DCM/MeOH 96:4) to give 27 mg of 3-fluoro-N-[3-(7-pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenyl]-benzenesulfonamide.
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08524707B2 |
| Quelldatensatz | uspto-grants-2013_09 |
| ORD ID | ord-66e88c0f0e00469c854c41e01f9ef212 |
| Quellennotiz | uspto-grants-2013_09 |