HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Diisopropylethylamine → (S)-2-amino-N-(1-(dimethylamino)-3-(4-isopropoxyphenyl)-1-oxopropan-2-yl)-4-(4-methylpiperazin-1-yl)quinazoline-7-carboxamide
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Diisopropylethylamine | HCID 81531 | — |
| Edukt | Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) | HCID 9886157 | — |
| Edukt | 2-Amino-4-(4-methylpiperazin-1-yl)quinazoline-7-carboxylic acid | HCID 59496649 | — |
| Edukt | (2S)-2-amino-3-(4-isopropoxyphenyl)-N,N-dimethylpropanamide | HCID 59496749 | — |
| Lösungsmittel | Dimethylformamide | HCID 6228 | — |
| Produkt | (S)-2-amino-N-(1-(dimethylamino)-3-(4-isopropoxyphenyl)-1-oxopropan-2-yl)-4-(4-methylpiperazin-1-yl)quinazoline-7-carboxamide | HCID 49779971 | 20% |
Reaktionsschritte
N,N,N′,N′-Tetramethyl-O-(7-azabenzotriazol-1-yl)uronium hexafluorophosphate (42 mg, 0.11 mmol) was added to a solution of 2-amino-4-(4-methylpiperazin-1-yl)quinazoline-7-carboxylic acid (20 mg, 0.07 mmol) in N,N-dimethylformamide (2 mL) and N,N-diisopropylethylamine (24 uL, 0.14 mmol). The reaction was stirred for 10 min, and the (2S)-2-amino-3-(4-isopropoxyphenyl)-N,N-dimethylpropanamide (35 mg, 0.14 mmol) was added. The reaction was stirred for 2 h. at r.t., and was purified by RP-HPLC (pH=2) to afford the desired product (7 mg, 20%) as a white solid TFA salt. Analytical LCMS (M+H)+: m/z=520.0.
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08481732B2 |
| Quelldatensatz | uspto-grants-2013_07 |
| ORD ID | ord-e1c537d695a342dc856cc47e43d70f89 |
| Quellennotiz | uspto-grants-2013_07 |