Reaktion #303947

Reaktionsgleichung

(8-methyl-2-(2-(trifluoromethyl)-phenyl)quinolin-3-yl)methanamine

iPr2NEt

6-chloropurine

→

N-((8-methyl-2-(2-(trifluoromethyl)phenyl)quinolin-3-yl)methyl)-9H-purin-6-amine

Lösungsmittel

EtOH

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigePrepared
2. 2
   SonstigeAfter purification, N-((8-methyl-2-(2-(trifluoro-methyl)phenyl)quinolin-3-yl)methyl)-9H-purin-6-amine as yellow syrup
3. 3
   SonstigeThe yellow syrup was triturated with CH2Cl2
4. 4
   Filtrationfiltered

Vorschrift

Prepared according to Procedure H using (8-methyl-2-(2-(trifluoromethyl)-phenyl)quinolin-3-yl)methanamine (0.1 g, 0.316 mmol, 1 eq) in EtOH (2 mL) was treated with iPr2NEt (0.07 mL, 0.4 mmol, 1.2 eq) followed by 6-chloropurine (0.049 g, 0.317 mmol, 1 eq). After purification, N-((8-methyl-2-(2-(trifluoro-methyl)phenyl)quinolin-3-yl)methyl)-9H-purin-6-amine as yellow syrup. The yellow syrup was triturated with CH2Cl2 and filtered to provide N-((8-methyl-2-(2-(trifluoromethyl)phenyl)quinolin-3-yl)methyl)-9H-purin-6-amine [PI3Kδ IC50=91 nM] as yellow syrup. 1H NMR (DMSO-d6) δ ppm 12.93 (1H, s), 7.98-8.31 (4H, m), 7.90 (1H, d, J=7.8 Hz), 7.74-7.82 (2H, m), 7.69 (2H, t, J=6.5 Hz), 7.59 (1H, d, J=7.0 Hz), 7.42-7.52 (1H, m), 4.42-4.77 (2H, m), 2.62 (3H, s). Mass Spectrum (ESI) m/e=435.1 (M+1).

Quelle