HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Hydrochloric Acid → 2-((2-(4-(Oxazol-5-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)(phenyl)amino)ethanol
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Hydrochloric Acid | HCID 313 | — |
| Edukt | Water | HCID 962 | — |
| Edukt | tert-butyl 4-((2-hydroxyethyl)(phenyl)amino)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate | HCID 59333719 | — |
| Lösungsmittel | Methanol | HCID 887 | — |
| Produkt | 2-((2-(4-(Oxazol-5-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)(phenyl)amino)ethanol | HCID 46200050 | 60% |
Reaktionsbedingungen
| Temperatur | 70 °C |
|---|
Reaktionsschritte
Hydrochloric acid (2 M, 2 ml) was added to a solution of tert-butyl 4-((2-hydroxyethyl)(phenyl)amino)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (150 mg, 0.28 mmol, Example 1a) in methanol (4 mL). Water (2 mL) was added and the solution was stirred at 70° C. for 30 min. The residual solvent was evaporated under reduced pressure and the crude product dissolved in DMSO. Purification by preparative HPLC afforded 2-((2-(4-(oxazol-5-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)(phenyl)amino)ethanol (72 mg, 54.8%). MS (ESI+)/(ESI−) m/z 429/427
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08188101B2 |
| Quelldatensatz | uspto-grants-2012_05 |
| ORD ID | ord-f81db7da34174f9c95a53ce6b562786d |
| Quellennotiz | uspto-grants-2012_05 |