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Benzaldehyde, 5-chloro-2-(1H-1,2,4-triazol-1-yl)- synthesis

2synthesis methods
-

Yield:1329166-77-9 41%

Reaction Conditions:

with caesium carbonate in dimethyl sulfoxide at 45; for 4 h;

Steps:

5-chloro-2-(lH-l,2,4-triazol-l-yl)benzaldehyde

5-chloro-2-fluorobenzaldehyde (1.29 g, 7.89 mmol), 4H-1,2,4-triazole (0.574 g, 7.89 mmol), Cs2CO3(2.83 g, 8.68 mmol) in DMSO (15.78ml) was capped and heated at 45°C for 4 hrs before cooling down to rt and stirred at rt over weekend. The reaction mixture was diluted with EtOAc, washed with water and brine, driedover MgSO4,filtered,concentrated. Purification by silica gel chromatography gave Intermediate 25A (674 mg, 41 % yield) as a white solid.

References:

JP2015/528022,2015,A Location in patent:Paragraph 0316