7-CHLORO-3-IODO (1H)INDAZOLE synthesis

Yield:885522-00-9 87.8%

Reaction Conditions:

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

Steps:

Preparation of 2-(3-carbamoyl-7-chloro-1H-indazol- 1-yl)acetic acid

To a mixture of 7-chloro-lH-indazole (0.6 g, 3.93mmol, 1.0 eq.), KOH (0.55 g, 9.8 mmol) in DMF was added I₂ (1.02g, 4.01 mmol, 1.02 eq.). The mixture was stirred at r.t. overnight, then quenched by aqueous Na₂S₂0₄ solution. The mixture was extracted with EtOAc (2 x 50 mL). The combined organic layers were dried over anhydrous Na₂S0₄ and concentrated. The resulting residue was purified by column chromatography (PE/EA =10: 1) to provide 7-chloro-3-iodo-lH-indazole (0.96 g, 87.8%).

References:

WO2018/229543,2018,A2 Location in patent:Paragraph 00207