Water → HCID 66719117, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of [1-(4-Bromo-phenyl)-3-hydroxy-3-methyl-cyclobutyl]-carbamic acid tert-butyl ester 2-1 (prepared according to WO2008/070041; 3.56 g, 10 mmol), Zn (1 g, 15 mmol), Zn(CN)2 (1.76 g, 15 mmol), Pd2(dba)3 (0.5 g, 0.5 mmol) and DPPF (300 mg, 0.5 mmol) in 30 mL of DMF was stirred at 100° C. for 2 hrs under N2. After the mixture was cooled to rt, 100 mL of water was added and product was extracted with ethyl acetate 100 mL×3. The organic layer was combined, washed with brine, dried over sodium sulfate and concentrated under vacuum. The residue was purified by silica gel chromatography using EA/PE (1:2) as eluant to give compound 2-2.

Provenance & Evidence