2-Aminothiazole → HCID 10020462, compound

Participants

Reaction Steps

A solution of (E)-3-cyclopentyl-2-(5-methylsulfanylpyridin-2-yl)acrylic acid (Preparation 5, 1.00 g, 3.8 mmol), EDCI (0.95 g, 4.9 mmol), HOBt (0.67 g, 4.9 mmol) and thiazol-2-ylamine (1.52 g, 15.2 mmol) in anhydrous THF (62 mL) and DMF (50 mL) was stirred at 20° C. for 4 d. The solvents were evaporated off under reduced pressure, then the residue was partitioned between CH2Cl2 and saturated aqueous Na2CO3. The organic layer was washed with H2O and brine, before being dried (MgSO4). Filtration, solvent evaporation, and column chromatography (7:31H-EtOAc) provided the title compound: RTA=3.96 min; m/z (ES+)=346.1 [M+H]+.

Provenance & Evidence