Yield:887351-37-3 86%

Reaction Conditions:

with triethylamine in N,N-dimethyl-formamide at 20;

Steps:

1.1

l,4-difluoro-2-nitrobenzene 9-a (CAS 364-74-9) ( 15 g, 94.3 mmol) was dissolved in DMF (500 mL). Cyclopropyl amine (7 mL, 100 mmol) was added followed by triethylamine (30 mL, 217 mmol). The resulting mixture was stirred at room temperature overnight. The mixture was poured in water and extracted with dichlorom ethane dried over MgS0₄ and concentrated. The orange solid was purified by column chromatography using dichloromethane and methanol to yield intermediate 9-b (16 g, 86%) as an orange solid.m/z = 197 (M+H)⁺. 1H NMR (400 MHz, CHLOROFORM-

References:

WO2012/80447,2012,A1 Location in patent:Page/Page column 20