Acetonitrile → HCID 67437567, compound

Participants

Reaction Steps

To 80 mg (0.15 mmol) of the aryl bromide, [(1S,2S)-1-({(4-bromo-phenyl)-[(trans)-2-(5-fluoro-pyridin-2-yl)-cyclopropanecarbonyl]-amino}-methyl)-2-methyl-butyl]-carbamic acid tert-butyl ester, in a microwave vial was added boronic acid (26 mg, 0.158 mmol), K2CO3 (41.5 mg, 0.301 mmol), PdCl2(PPh3)2 (5.3 mg, 0.008 mmol), 6 mL of MeCN, and 1 mL of water. The resulting mixture was microwaved at 140° C. for 30 min. It was then diluted with EtOAc, washed with water, brine and concentrated, and then purified in the neutral PREP HPLC to give 62 mg (72%) of the desired product.

Provenance & Evidence