N-(5-amino-4-fluoro-2-methylphenyl)acetamide → N-[5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]-4-fluoro-2-methylphenyl]acetamide

Temperatur

150 °C

In 20 ml microwave vial were added 5-chloro-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile (200 mg, 0.86 mmol), N-(5-amino-4-fluoro-2-methylphenyl)acetamide (164 mg, 0.90 mmol), Pd2dba3 (39.2 mg, 0.04 mmol), di-tert- butyl(2',4',6'-triisopropylbiphenyl-2-yl)phosphine (37.5 mg, 0.09 mmol) and Cs2CO3 (837 mg, 2.57 mmol). The vessel was fitted with septum, gas inlet and dioxane (8 mL) was added via syringe. The resulting suspension was stirred for 5 min. under N2. The septum and gas inlet quickly replaced with microwave vial cap and the mixture was heated to 150oC under microwave irradiation for 30 min. The reaction mixture filtered through celite, filtrate concentrated, combined with EN02368-53 experiment and purified by ISCO column (0-5% MeOH-CH2Cl2). The obtained compound triturated with CH3CN, filtered and dried to give light brown color solid. Conclusion: product isolated

ORD-Eintrag

ord-71ad501d78264f9aa8b8fb6c66e7e044

Quelldatensatz

750 AstraZeneca ELN dataset

Originallink

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