7-methoxyquinoline-8-carboxylic acid synthesis

Yield:1159427-80-1 35%

Reaction Conditions:

in 1,4-dioxane at 200; for 0.333333 h;Microwave irradiation;

Steps:

1.1a

N-rf7-hvdroxy-8-quinolinyl)carbonyl1glvcine; Ia) 7-(methyloxy)-8-quinormecarboxylic acid; A mixture of 2-amino-6-(methyloxy)benzoic acid (1.00 g, 6.00 mmol) and acrolein (0.445 mL, 6.00 mmol) in 1,4-dioxane (6.0 mL) was heated to 200 ⁰C for 20 min. in a Biotage Initiator microwave synthesizer (http://www.biotage.com). The mixture was concentrated in vacuo and purified via flash column chromatography (0-10% methanol in dichloromethane) to afford the title compound (0.430 g, 35%) as a light orange solid. ¹H NMR (400 MHz, DMSO-

References:

WO2009/70644,2009,A1 Location in patent:Page/Page column 14