4,6-DIFLUORO-3-IODOINDAZOLE synthesis
- Product Name:4,6-DIFLUORO-3-IODOINDAZOLE
- CAS Number:887567-79-5
- Molecular formula:C7H3F2IN2
- Molecular Weight:280.01
885520-26-3
887567-79-5
Example 10: Synthesis of 1.2-(4,6-difluoro-1-methyl-1H-indazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxyisopropylamide Step 1: Synthesis of 4,6-difluoro-3-iodo-1H-indazole At room temperature, 4,6-difluoro-1H-indazole (1.16 g, 7.53 mmol) was dissolved in DMF (60 mL) and potassium hydroxide (1.27 g, 22.6 mmol) and iodine (2.87 g, 11.3 mmol) were added sequentially. The reaction mixture was stirred at room temperature for 2 h. The reaction solution was maroon in color. After completion of the reaction, the reaction was quenched with 10% Na2S2O3 aqueous solution and diluted with water. The mixture was extracted with EtOAc (2×). The organic phases were combined, washed sequentially with water, saturated LiCl solution and saturated NaCl solution, dried over MgSO4 and concentrated to give 4,6-difluoro-3-iodo-1H-indazole (2.18 g) as a light brown solid.
885520-26-3
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887567-79-5
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$57.00/100mg
Yield:887567-79-5 2.18 g
Reaction Conditions:
with iodine;potassium hydroxide in N,N-dimethyl-formamide at 20; for 2 h;
Steps:
101.1 Step 14 ,6 -Difluoro -3 -iodo - 1 H-indazo le
Example 101.2-(4,6-Difiuoro-l-methyl-lH-indazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylisopropylamideStep 14 ,6 -Difluoro -3 -iodo - 1 H-indazo leTo a solution of 4,6-difluoro-l H-indazo le (1.16 g, 7.53 mmol) in DMF (60 ml) at room temperature was added potassium hydroxide ( 1.27 g, 22.6 mmol) and iodine (2.87 g, 11.3 mmol). The maroon reaction mixture was stirred at room temperature for 2 h then quenched with 10% aqueous Na2S203 and diluted with water. The mixture was extracted with EtOAc (2x). The combined organics were washed with water, sat LiCl, and sat NaCl, then dried over MgSC^ and concentrated to afford 2.18 g of 4,6-difluoro-3-iodo-l H-indazo le as a light brown solid.
References:
WO2013/30138,2013,A1 Location in patent:Page/Page column 262; 263
58551-83-0
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887567-79-5
28 suppliers
$57.00/100mg