4-Chlorocinnoline → HCID 90682467、化合物

反応式

Clc1cnnc2ccccc12.Cn1ncc(C(=O)N2CCC(N)CC2)c1Cl>CC(=O)O.CC(=O)O.Cc1ccccc1.O=C([O-])[O-].[Cs+].[Cs+].[Pd].c1ccc(P(c2ccccc2)c2ccc3ccccc3c2-c2c(P(c3ccccc3)c3ccccc3)ccc3ccccc23)cc1>Cn1ncc(C(=O)N2CCC(Nc3cnnc4ccccc34)CC2)c1Cl

参加物

反応条件

温度: 140 °C

実験手順

(4-aminopiperidin-1-yl)(5-chloro-1-methyl-1H-pyrazol-4-yl)methanone (442 mg, 1.82 mmol) was taken in a microwave tube. Added racemic-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (113 mg, 0.18 mmol) followed by the addition of Palladium (II) acetate (40.9 mg, 0.18 mmol), racemic-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (113 mg, 0.18 mmol), Cesium carbonate (1782 mg, 5.47 mmol) and diisopropylethyl amine(1ml). toluene (10 mL) was added and stirred at 140 °C for 8h. After the completon of the reaction adsorbed the reaction mass on silica gel and purified by silica gel column.