Potassium Phosphate, Tribasic → HCID 86703777, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of product from step 1 (29.1 mg), cyclopropylboronic acid (31.4 mg), potassium phosphate (188 mg), palladium acetate (2.8 mg) and tricyclohexylphosphine tetrafluoroborate (8.8 mg) in toluene (1.2 mL) and water (0.06 mL) was heated at 95° C. for 16 hours. The contents were concentrated. The residue was diluted with EtOAc and washed with 1M NaH2PO4 and brine, and dried (Na2SO4). After filtration and concentration, the crude was purified with HPLC (10.3 mg). LCMS (Method D): RT=5.44 min, m/z: 509.2 [M+H]+. 1H NMR (400 MHz, DMSO-d6) δ 11.78 (s, 1H), 7.46-7.38 (m, 4H), 7.29 (t, J=7.5 Hz, 4H), 7.18 (dd, J=18.0, 7.9 Hz, 3H), 6.96 (d, J=12.9 Hz, 1H), 4.54 (s, 1H), 4.22 (d, J=6.2 Hz, 2H), 3.07 (s, 2H), 2.89 (s, 1H), 2.13-1.98 (m, 1H), 0.96-0.83 (m, 2H), 0.72-0.61 (m, 2H).

Provenance & Evidence