Formaldehyde → 2-[1,1'-Biphenyl]-4-yl-3-(dimethylamino)-6-fluoro-4-quinolinecarboxylic acid

참여 물질

반응 조건

반응 단계

A 4 g portion of 3-amino-2-[1,1'biphenyl]-4-yl-6-fluoro-4-quinolinecarboxylic acid was dissolved in 250 ml of acetonitrile. To this was added 2.7 ml of 40% aqueous formaldehyde and the mixture was heated at 80° C. until solution was complete. A 2.1 g portion of sodium cyanoborohydride was added and the solution stirred at 20° C. for 8 hours. Glacial acetic acid was added to pH 6, then 0.69 g of sodium borohydride was added and stirring continued at 20° C. for 72 hours. The reaction mixture was poured into 1 liter of water and adjusted to pH 4 with glacial acetic acid. The solid was collected, washed with water, dried and then twice suspended in 200 ml of hot ethanol and filtered. The solid was collected, giving 2.5 g of the desired product as a yellow powder, mp 235°-239° C. (gas solution).

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