反应详情

温度

125 °C

The intermediate 7-chloro-3-{[(6-chloro-pyridine-3-carbonyl)-amino]-methyl}-4-oxo-1-phenyl-1,4-dihydro-quinoline-2-carboxylic acid dimethylamide (70 mg, 0.141 mmol) was combined with piperidin-4-ylmethanol (40 mg, 0.346 mmol) and NMP (2 mL). The reaction mixture was heated at 125° C. for 2 hr. After this time, the crude product was subjected to preparative reverse-phase HPLC purification. The product, 4-hydroxymethyl-3,4,5,6-tetrahydro-2H[1,2′]bipyridinyl-5′-carboxylic acid (7-chloro-2-dimethylcarbamoyl-4-oxo-1-phenyl-1,4-dihydro-quinolin-3-ylmethyl)-amide was obtained as 30 mg (37%) of a white solid. MS calcd. for C31H32ClN5O4 [(M+H)+] 574.2, obsd. 574.3.

1. customAfter this time, the crude product was subjected to preparative reverse-phase HPLC purification