Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|
| Edukt | Potassium Carbonate | HCID 11430 | — |
| Edukt | (3Z)-1-Cyclopropyl-4-(dimethylamino)-3-[2-(pyridin-4-ylamino)pyrimidin-4-yl]but-3-en-2-one | HCID 67983720 | — |
| Edukt | HCID 178459320 | HCID 178459320 | — |
| Lösungsmittel | Dimethylformamide | HCID 6228 | — |
| Produkt | VPS34 inhibitor 1 | HCID 67983918 | 39% |
Reaktionsschritte
To a solution of (Z)-1-cyclopropyl-4-(dimethylamino)-3-(2-(pyridin-4-ylamino)pyrimidin-4-yl)but-3-en-2-one (9) (50 mg, 0.155 mmol) in DMF (1288 μl), 1-(2-hydroxy-2-methylpropyl)guanidine and potassium carbonate (107 mg, 0.773 mmol) were added and the reaction mixture was stirred at 120° C. for 2 hours. The crude product was purified by reverse-phase HPLC [30-90% organic phase over 15 minutes] followed by Biotage™ silica gel chromatography [10 g SNAP column, 100% DCM to 12% MeOH/DCM] to obtain the desired product (23.8 mg, 39%).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patentnummer | US08901147B2 |
|---|
| Quelldatensatz | uspto-grants-2014_12 |
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| ORD ID | ord-d25aa6369bc74bbc80f1a6680e086a0c |
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| Quellennotiz | uspto-grants-2014_12 |
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