Triethylamine → 7-[(2,4-Dichloro-3-fluorophenyl)carbonyl]-3-(1,2,4-thiadiazol-5-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine

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Reaction Steps

A mixture of 3-(1,2,4-thiadiazol-5-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine (I115) (30 mg, 0.144 mmol) and triethylamine (0.030 mL, 0.216 mmol) in Dichloromethane (DCM) (2 mL) was stirred at room temperature. 2,4-Dichloro-3-fluorobenzoyl chloride (36.0 mg, 0.158 mmol) in DCM (0.5 ml) was added and stirring continued at room temperature. After 30 mins, 2 drops MeOH were added followed by sat. NaHCO3 solution (3 ml) and ethyl acetate (30 ml). The product was extracted into the ethyl acetate which was dried (Na2SO4) and concentrated. The product was purified by high pH MDAP to give desired product as a white solid after evaporation of the fractions.

Provenance & Evidence