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

Participants

Reaction Steps

570 mg (4.12 mmol) of potassium carbonate are added to a suspension of 560 mg (2.06 mmol) of 5-(3-chloro-4-methyl-2-thienyl)-4-isobutyl-2,4-dihydro-3H-1,2,4-triazol-3-one from Example 247A and 253 mg (2.06 mmol) of ethyl chloroacetate in 10 ml acetonitrile and heated for 4 hrs under reflux. For the workup, this is concentrated, and the residue taken up in water and extracted three times with ethyl acetate. The combined organic phases are concentrated, and the crude product remaining as the residue is purified by preparative HPLC [Method 12]. 705 mg (96% of theory) of the target compound are thus obtained.

Provenance & Evidence