تفاعل #325
ord-f1632d43480c447bab6a25aa93c74396
معادلة التفاعل
CN1Cc2ccc(Cl)nc2O[C@
COc1cc(N)ccc1-n1cnc(
→
COc1cc(Nc2ccc3c(n2)O
المردود 19.0%
المذيبات
ظروف التفاعل
درجة الحرارة
100°CELSIUS
الإجراء التجريبي
(R)-8-chloro-4-methyl-2-phenyl-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepine (180 mg, 0,66 mmol), 3-methoxy-4-(3-methyl-1H-1,2,4-triazol-1-yl)aniline (134 mg, 0,66 mmol), Palladium acetate (14,71 mg, 0,07 mmol), 2-(Dicyclohexylphosphino)biphenyl (22,96 mg, 0,07 mmol) and Cesium carbonate (640 mg, 1,97 mmol) were mixed in DME (3 mL) in a microwave vial. EtOH (0,3 mL) was added and the mixture was run for 1 hour at 100°C in a microwave reactor. the reaction had to be run for an additional 2 hours with more catalyst and ligand added. the mixture was filtered and purified using flash chromatography 0-10% MeOH in DCM.
المصدر
750 AstraZeneca ELN dataset