HCID 86623153, compound → HCID 11998799, compound

Participants

Reaction Conditions

Reaction Steps

To N-{5-[2-Bromo-5-(4-hydroxy-piperidine-1-sulfonyl)-thiophen-3-yl]-4-methyl-thiazol-2-yl}-acetamide obtained in Step I as described above (3500 mg; 6.27 mmol; 1 eq), is dissolved in anhydrous THF (150 ml). The reaction mixture is cooled down to −70° C. and put under nitrogen. n-Butyllithium (18.8 ml; 1.6 M; 37.6 mmol; 6 eq) is added dropwise. The reaction is stirred over weekend and is quenched with water. Solvents are evaporated and the resulting crude product is dissolved in EtOAc, washed with water (2 times), brine and dried over MgSO4. After evaporation of the solvents, the resulting product is suspended in ACN and filtered, affording Compound (39) as a beige solid (830 mg; 32%).

Provenance & Evidence