Boron tribromide dichloromethane → Ethyl 2-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-4-(hydroxymethyl)-1,3-thiazole-5-carboxylate

Participants

Reaction Conditions

Reaction Steps

Ethyl 2-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-4-(methoxymethyl)-1,3-thiazole-5-carboxylate (Example 276; 50 mg; 0.105 mmol) was dissolved in anhydrous DCM and cooled to −78° C. 1 M Boron tribromide/DCM (105 μl; 0.105 mmol) was added dropwise. The mixture was stirred at −78° C. for 15 min, then at room temperature for 4 h. The mixture was diluted with DCM, washed with water and dried over Na2SO4. Organic phase was concentrated in vacuo giving the title compound (20 mg).

Provenance & Evidence