반응 #401

ord-92bacb0740454b4398d7f3969518ce26

반응 방정식

NC(=O)c1ccc(Cl)nc1
NC(=O)c1ccc(Cl)nc1
NCc1ccc(C(F)(F)F)cc1
NCc1ccc(C(F)(F)F)cc1
NC(=O)c1ccc(NCc2ccc(C(F)(F)F)cc2)nc1
NC(=O)c1ccc(NCc2ccc(
수율 7.4%

용매

반응 조건

온도
100°CELSIUS

실험 절차

To a stirred solution of 6-chloronicotinamide (0.053 g, 0.34 mmol), 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (0.021 g, 0.03 mmol), sodium 2-methylpropan-2-olate (0.065 g, 0.68 mmol) and diacetoxypalladium (7.60 mg, 0.03 mmol) in DME (1 mL) was added (4-(trifluoromethyl)phenyl)methanamine (0.097 mL, 0.68 mmol). The reaction was run in microwave at 100 °C for 4h. The compound was purified by preparative HPLC on a Kromasil C8 column (10 µm 250x20 ID mm) using a gradient of 51-55% acetonitrile in H2O/ACN/FA 95/5/0.2 buffer, over 25 minutes with a flow of 19 mL/min. The compounds were detected by UV at 270nm. 6-(4-(trifluoromethyl)benzylamino)nicotinamide (7.40 mg, 7.40 %) was obtained.

출처

750 AstraZeneca ELN dataset