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635713-71-2

1-N-BOC-5-FORMYL-INDAZOLE synthesis

1synthesis methods
253801-04-6 Synthesis
1H-INDAZOLE-5-CARBALDEHYDE

253801-04-6
161 suppliers
$26.00/250mg

24424-99-5 Synthesis
Di-tert-butyl dicarbonate

24424-99-5
825 suppliers
$13.50/25G

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Yield:635713-71-2 99%

Reaction Conditions:

dmap in acetonitrile at 20; for 0.5 h;

Steps:



5-Formyl-indazole-1-carboxylic acid tert-butyl ester (58) To a solution of 57 (0.21 g, 1.43 mmol) in acetonitrile (10 ml) was added BOC anhydride (0.314 g, 1.43 mol) followed by catalytic amounts OF DMAP (0.03 g). After 30 minutes of stirring at room temperature, solvent was evaporated, EtOAc (30 ml) was added and the organic layer was washed with 0.5 N HCl solution (10 ml) and brine. It was then dried (NA2S04) and concentrated to give 0.35 g (99% yield) desired product that was used to prepare di-Boc-protected 3 without purification.

References:

WO2005/813,2005,A1 Location in patent:Page 37

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