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Method of synthesising quinoline D.57Ethoxyacrylate ED.13 (6.4 mL, 44.3 mmol) is placed in MeOH (120 mL), combined with HCI (88 mL, 2M in H20) and heated to 100°C. Benzaldehyde ED.12 (4.00 g, 20.1 mmol) is placed in MeOH (120 mL), slowly added dropwise to the reaction mixture and the reaction mixture is heated to 100°C for 4 h. Then it is made basic with NaHC03, the solvent is eliminated, the residue is purified by chromatography (90:10 to 40:60 in 15 min hexane/EtOAc) and quinoline D.57 (4.08 g, 51 percent; HPLC-MS: MS(M+H)+ = 266/268; tRet = 1 .50 min; method LCMSBAS1 ) is obtained.
With hydrogenchloride; In methanol; water; at 100℃; for 4h;
Method of Synthesising Quinoline D.57Ethoxyacrylate ED.13 (6.4 mL, 44.3 mmol) is placed in MeOH (120 mL), combined with HCl (88 mL, 2M in H2O) and heated to 100° C. Benzaldehyde ED.12 (4.00 g, 20.1 mmol) is placed in MeOH (120 mL), slowly added dropwise to the reaction mixture and the reaction mixture is heated to 100° C. for 4 h. Then it is made basic with NaHCO3, the solvent is eliminated, the residue is purified by chromatography (90:10 to 40:60 in 15 min hexane/EtOAc) and quinoline D.57 (4.08 g, 51percent; HPLC-MS: MS (M+H)+=266/268; tRet=1.50 min; method LCMSBAS1) is obtained.
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