تفاعل #396

ord-916b542fdcc44d6284100092f1e92c3f

معادلة التفاعل

Cc1cc(Cl)nc2c1CN(C)CC(CC(F)(F)F)O2
Cc1cc(Cl)nc2c1CN(C)C
COc1nc(N)ccc1-c1cnn(C)c1
COc1nc(N)ccc1-c1cnn(
COc1nc(Nc2cc(C)c3c(n2)OC(CC(F)(F)F)CN(C)C3)ccc1-c1cnn(C)c1
COc1nc(Nc2cc(C)c3c(n
المردود 9.8%

المذيبات

ظروف التفاعل

درجة الحرارة
100°CELSIUS

الإجراء التجريبي

6-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-amine (104 mg, 0.51 mmol), 8-chloro-4,6-dimethyl-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepine (150 mg, 0.51 mmol), Sodium tert-butoxide (73.4 mg, 0.76 mmol), rac-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (22.19 mg, 0.04 mmol) and Tris(dibenzylideneacetone)dipalladium(0) (32.6 mg, 0.04 mmol) were added to a radley tube followed by toluene (6 mL). The reaction mixture was flushed with argon and the mixture was heated to 100°C and stirred overnight. The solids were filtered off and washed with DCM. The crude product was purified on prepHPLC yielding N-(6-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-4,6-dimethyl-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepin-8-amine (23.00 mg, 9.77 %)

المصدر

750 AstraZeneca ELN dataset