Phosphoric Acid → HCID 10133523, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-[4-(1-ethyl-propylamino)-6-methyl-2-(2,4,6-trimethyl-phenoxy)-pyridin-3-ylmethyl]-malonic acid diisopropyl ester (40 mg, 0.078 mmol) and 85% phosphoric acid was heated at 73° C. overnight, and then heated at 133° C. for 1 hour. The reaction mixture was cooled, quenched with water and extracted with ethyl acetate. The organic layer was washed with brine, dried and concentrated to give a brown oil. The oil residue was purified through silica gel column chromatography using 3% ethyl acetate in hexane as eluent to give 28 mg (98%) of the title compound. 1H NMR (CDCl3) δ 6.89(s,2H), 6.56(s,1H), 4.4(m,1H), 3.00(m,2H), 2.67(m,2H), 2.31(s,3H), 2.25(s,3H), 2.07(s,6H), 1.86(m,4H), 0.90(t,6H) ppm.

Provenance & Evidence