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

Yield:847906-27-8 92%

Reaction Conditions:

with iodine;potassium hydroxide in N,N-dimethyl-formamide at 20; for 4 h;

Steps:

619.1 Step 1

A solution of 7-methyl-1H-indazole (2 g, 15.15 mmoL), KOH (2.12 g, 37.88 mmoL) and ‘2 (7.7 g, 30.3 mmoL) in DIVIF (40 mL) was stirred at room temperature for 4 hrs. The reaction mixture was poured into H20 (200 mL) and extracted with EA (200 mL). The EA layer was washed with saturated NaSO3 (100 mL), H20 (200 mL), brine (200 mL), dried over Na2SO4 and concentrated to give 3-iodo-7-methyl-1H-indazole (3.6 g, yield: 92%) as a yellow solid.

References:

WO2018/132372,2018,A1 Location in patent:Paragraph 01237