Реакция #829

ord-e0d4157f08c0492097a16f50798a4aa4

Уравнение реакции

N#Cc1cnn2c(NC3CC3)cc(Cl)nc12
N#Cc1cnn2c(NC3CC3)cc
OCc1ccc2cc[nH]c2c1
OCc1ccc2cc[nH]c2c1
N#Cc1cnn2c(NC3CC3)cc(-n3ccc4ccc(CO)cc43)nc12
N#Cc1cnn2c(NC3CC3)cc
Выход 47.5%

Растворители

Условия реакции

Температура
150°CELSIUS

Методика

In a 40mL vial (t=g) was 5-chloro-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile (50 mg, 0.21 mmol), [Reactants], and cesium carbonate (77 mg, 0.24 mmol) in DMA (0.5 mL) ([VOLUME]),Pd2(dba)3 (9.80 mg, 10.70 µmol) and (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (12.38 mg, 0.02 mmol) were added. to give a brown suspension. The vial was filled with N2, 150C microwave for 30 min. LCMS showed completion. added MeOH (3 mL), filtered through celite. concentrated. The residue was purified by ISCO (Hexane to EtOAc:Hex=1;1 to EtOAc) to give about 34 mg offwhite solid

Источник

750 AstraZeneca ELN dataset