4-CYANO-3-IODO (1H)INDAZOLE synthesis

Yield:944898-93-5 64.7%

Reaction Conditions:

with iodine;potassium hydroxide in N,N-dimethyl-formamide at 20;

Steps:

17.2

step 2: A mixture of lH-indazole-4-carbonitrile (1.65g, 11.1 mmol), KOH (1.86 g, 33.3 mmol), and (5.6 g, 22.2 mmol) in DMF (30 mL) was stirred at RT overnight. The reaction mixture was filtered. The filtrate was diluted with water (100 mL) and extracted with EtOAc (200 mL). The organic layer was concentrated in vacuo to afford 3-iodo-lH-indazole-4-carbonitrile as white solid (2.01 g, 64.7%). MS (ESI): w/z = 270 [M+l]+.

References:

WO2013/26914,2013,A1 Location in patent:Page/Page column 112