Ethyl chloroacetate → Ethyl [3-(5-chloro-2-thienyl)-4-(2-methoxyethyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl]acetate

Participants

Reaction Conditions

Reaction Steps

2.4 g (9.24 mmol) of the compound of Example 50A and 2.55 g (18.48 mmol) of potassium carbonate were suspended in 48 ml of acetonitrile. 1.08 ml (10.17 mmol) of ethyl chloroacetate were then added, and the mixture was heated under reflux at 80° C. for 4.5 h. Another 113 mg (0.92 mmol) of ethyl chloroacetate were then added, and the mixture was stirred at 80° C. for a further 2 h. The suspension was then filtered through a layer of silica gel and washed with ethyl acetate, the filtrate was evaporated on a rotary evaporator and the residue was dried under high vacuum. This gave 3.24 g (100% of theory) of the title compound.

Provenance & Evidence