Study on the synthesis process and stability of anti-influenza virus indoloquinoline boronic acid compound IQB-6
Objective To study synthesis process,solubility and stability of IQB-6,an indole quinolineboronic acid candidate compound with excellent in vitro and in vitro anti-influenza virus activity discovered by our research group.Methods Firstly,for purpose of improving the yield and purity of IQB-6,a series of reaction conditions were optimized by controlling the material feeding ratio,solvent volume,reaction time,reaction temperature,post-treatment and purification methods.Secondly,the solubility of IQB-6 in eight solvents such as n-hexane,water,ethanol and DMSO was tested.Finally,the stability of IQB-6 solid under high temperature,high humidity,light,acid,alkali and oxidation conditions was investigated,and the stability of IQB-6 solid in artificial gastric and intestinal fluids,plasma of SD rats was tested.Results The IQB-6 product with purity greater than 99％was obtained through seven steps,and the overall yield was 25％.Studies on the solubility of IQB-6 in organic solvents mentioned above showed that the solubility of IQB-6 in DMSO was the best and that in water was the worst,and it only had a certain solubility in others.In addition,stability studies under high temperature,high humidity,light and other conditions found that IQB-6 solid had a certain stability.Conclusion The optimized process had the advantages of low cost,simple operation and simple amplification.The dissolution characteristics of IQB-6 could provide guidance for further preparation research.The physical and chemical properties of IQB-6 were stable,which was convenient for storage,transportation and administration.The relevant stability test could provide certain guidance for the later quality standard and drug metabolism research.
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