Cyclopropylboronic acid → HCID 57744441, compound

Participants

Reaction Steps

Following the procedure as described in Example 19, making variations only as required to use cyclopropylboronic acid in place of phenethylboronic acid to react with -(5-(benzylcarbamoyl)-4-methylthiazol-2-yl)-2-oxo-1,2-dihydropyridin-4-yl trifluoromethanesulfonate, the title compound was obtained as a colorless solid in 54% yield: mp 149-151° C. (ethyl acetate/hexanes); 1H NMR (300 MHz, CDCl3) δ 8.63 (d, J=7.6 Hz, 1H), 7.39-7.25 (m, 5H), 6.39 (d, J=1.5 Hz, 1H), 6.10-6.05 (m, 2H), 4.58 (d, J=5.6 Hz, 2H), 2.69 (s, 3H), 1.81-1.72 (m, 1H), 1.14-1.07 (m, 2H), 0.86-0.81 (m, 2H); 13C NMR (75 MHz, CDCl3) δ 162.2, 160.3, 158.8, 153.4, 152.3, 137.7, 130.3, 128.8, 127.9, 127.6, 127.7, 114.7, 106.6, 44.1, 17.3, 15.4, 10.4; MS (ES+) m/z 366.1 (M+1).

Provenance & Evidence