HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
1,2-Diaminocyclohexane, trans- → 1-Benzothiazol-6-yl-3-(4-trifluoromethyl-pyridin-3-yl)-imidazolidin-2-one
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | 1,2-Diaminocyclohexane, trans- | HCID 43806 | — |
| Edukt | Potassium Phosphate, Tribasic | HCID 62657 | — |
| Edukt | 3-Bromo-4-(trifluoromethyl)pyridine | HCID 19937263 | — |
| Edukt | 1-Benzothiazol-6-yl-imidazolidin-2-one | HCID 66678554 | — |
| Katalysator | Copper iodide | HCID 83717 | — |
| Lösungsmittel | 1,4-Dioxane | HCID 31275 | — |
| Produkt | 1-Benzothiazol-6-yl-3-(4-trifluoromethyl-pyridin-3-yl)-imidazolidin-2-one | HCID 49872356 | 12,04% |
Reaktionsschritte
Using the same reaction conditions as in Example 14, 1-benzothiazol-6-yl-imidazolidin-2-one (I-84b: 150 mg, 0.684 mmol) was reacted with 3-bromo-4-trifluoromethyl-pyridine (185.75 mg, 0.822 mmol), 1,4-dioxane (10 mL), copper iodide (12.99 mg, 0.0684 mmol), trans-1,2-diamino cyclohexane (23.37 mg, 0.205 mmol) and potassium phosphate (435 mg, 2.052 mmol) to afford the crude product. Purification by column chromatography on silica gel (1% MeOH in CHCl3), followed by preparative HPLC afforded 7 mg of the product (12.04% yield).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | USRE045173E1 |
| Quelldatensatz | uspto-grants-2014_09 |
| ORD ID | ord-535264ea86a441f281b9f18678908f26 |
| Quellennotiz | uspto-grants-2014_09 |