تفاعل #566

ord-067637c197bb4672875d64a38b7940ee

معادلة التفاعل

Cc1ccc(Oc2ccnc(Cl)c2)c(C)n1
Cc1ccc(Oc2ccnc(Cl)c2
COCC(C)NS(=O)(=O)c1ccc(N)cc1
COCC(C)NS(=O)(=O)c1c
COCC(C)NS(=O)(=O)c1ccc(Nc2cc(Oc3ccc(C)nc3C)ccn2)cc1
COCC(C)NS(=O)(=O)c1c
المردود 52.0%

المذيبات

ظروف التفاعل

درجة الحرارة
150°CELSIUS

الإجراء التجريبي

In a 10 mL microwave reactor 3-(2-chloropyridin-4-yloxy)-2,6-dimethylpyridine (100 mg, 0.43 mmol) and 4-amino-N-(1-methoxypropan-2-yl)benzenesulfonamide (104 mg, 0.43 mmol) were dissolved in DMA (3 mL) to give a brown solution.To the resultant solution Cesium carbonate (0.068 mL, 0.85 mmol) was added and sparged with nitrogen for 1 minute. Then Palladium(II) acetate (6.70 mg, 0.03 mmol) and 9,9-Dimethyl-4,5-bis(diphenylphosphino)xanthene (29.6 mg, 0.05 mmol) were added and the reaction mixture was sealed. The reaction was heated to150 °C for 25 minutes in the biotage microwave.The reaction was cooled to room temperature and LCMS shows reaction was completed. Reaction mixture was filtered through Celite Bed and washed with Dichloromethane. Filtrate was subjected to concentration to get DMA solution which was given to analytical department to purify using Mass based HPLC. After purification compound was isolated to get pale yellow solid of 4-(4-(2,6-dimethylpyridin-3-yloxy)pyridin-2-ylamino)-N-(1-methoxypropan-2-yl)benzenesulfonamide (98 mg, 52.0 %)

المصدر

750 AstraZeneca ELN dataset