Toluene → HCID 58787888, compound

Participants

Reaction Conditions

Reaction Steps

(R)-2-tert-Butoxycarbonylamino-2-methyl-4-(4-trifluoromethane sulfonyloxy-phenyl)-butyric acid ethyl ester (100 mg), 4-butylboronic acid (75 mg) and K2CO3 (44 mg) are suspended in dry toluene (3 ml). Argon is bubbled through the mixture for 10 min., tetrakispalladiumtriphenyl-phosphine (5 mg) is added and the mixture is stirred at 95° C. under Argon for 16 h. After cooling to RT, ethyl acetate (5 ml) is added and the mixture is washed with 0.5N NaOH (2 ml), water (2 ml), 1M citric acid (2×2 ml) and water (2 ml). The organic phase is dried over MgSO4, the solvent removed and the crude material purified by chromatography using diethylether/hexane=1/5 (Rf=0.14, MS: (ES+): 454.6 (M+H)+).

Provenance & Evidence