Related Products of 1128-00-3,Some common heterocyclic compound, 1128-00-3, name is Ethyl 2-aminocyclohex-1-enecarboxylate, molecular formula is C9H15NO2, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
To a solution of 170 mg of ethyl 2-aminocyclohex-1-enecarboxylate as synthesized in Step 7-1-B in 5 ml of pyridine, 70 mg of phosphorus trichloride was added under cooling with ice, followed by 15 minutes’ stirring. Raising the temperature to room temperature, 327 mg of 5-(4-quinoline-2-ylpiperazin-1-yl)hexanoic acid as synthesized in above Step 7-14-C was added to the solution and stirred for 3 hours. Distilling the pyridine off under reduced pressure, the residue was extracted with ethyl acetate and washed with water. The organic layer was dried over anhydrous magnesium sulfate, and the solvent was concentrated under reduced pressure. The residue was purified on silica gel column chromatography (ethyl acetate) to provide 182 mg (38%) of ethyl 2-[5-(4-quinolin-2-ylpiperazin-1-yl)hexanoylamino]cyclohex-1-enecarboxylate. 1H-NMR(CDCl3)delta:11.61(br s,1H),7.86(d,J=8.9Hz,1H), 7.68(d,J=8.5Hz,1H),7.57(d,J=7.7Hz,1H), 7.51(ddd,J=1.2Hz,6.9Hz,8.1Hz,1H),7.22~7.18(m,1H), 6.96(d,J=9.3Hz,1H),4.14(q,J=6.9Hz,2H),3.80~3.70(m,4H), 2.98~2.95(m,2H),2.75~2.65(m,3H),2.64~2.56(m,2H), 2.34(t,J=7.3Hz,2H),2.31~2.28(m,2H),1.81~1.70(m,2H), 1.69~1.56(m,6H),1.26(t,J=6.9Hz,3H),1.01(d,J=6.6Hz,3H) Mass,m/e:478(M+),157(base)
The synthetic route of 1128-00-3 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ASKA Pharmaceutical Co., Ltd.; EP1724267; (2006); A1;,
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