The synthesis process optimization of 1(- 4-aminophenyl)-5, 6-dihydro-3- (4-morpholinyl)-2(1H)-pyridinone, an important intermediate for the apixaban synthesis / 国际药学研究杂志

Objective: To optimize the synthesis process of 1-(4-aminophenyl)-5, 6-dihydro-3-(4-orpholinyl)-2(1H)-pyridinone.Methods: Using p-nitroaniline as the raw material, the target compound was obtained by amidation, cyclization, chlorination, nitration and reduction reactions. The sodium hydride catalyst for cyclization was taken out in the reaction, the reaction acid binding agent was improved, the reaction temperature of intermediate was reduced, the optimal ratio and reaction ratio condition were investigated, and the post-processing conditions were optimized for each reaction. Results: The target compound was confirmed by 1H NMR and 13C NMR data, and the total yield was 65.4%. Conclusion: The optimized process is simple to operate, mild and controllable, and the solvent is easy to recycle, low-polluting and more conducive to industrial production.

Fluorescent Detection of p-Nitroaniline Based on an Anionic Pyrenyl Probe / 分析化学

p-Nitroaniline ( PNA) was one kind of highly toxic aromatic amine and becomes an environmental pollutant in recent years. Here we reported the construction of a fluorescent sensor based on an anionic pyrene, 8-hydroxypyrene-1,3,6-trisulfonic acid trisodium salt (HPTS), for the rapid and visual detection of PNA in aqueous media. The fluorescence quenching of HPTS caused by the presence of PNA was through non-covalent interactions. A good linear relationship between fluorescent intensity of HPTS at 512 nm was obtained in the range of 10-120 μmol/L. The detection limit (3σ) of this approach was 4. 6 μmol/L. The results showed that the method was suitable for rapid detection of PNA in real samples with good sensitivity, selectivity, anti-interference, low cost and easy operation.

Fluorescent Detection of p-Nitroaniline Based on an Anionic Pyrenyl Probe / 分析化学

p-Nitroaniline ( PNA) was one kind of highly toxic aromatic amine and becomes an environmental pollutant in recent years. Here we reported the construction of a fluorescent sensor based on an anionic pyrene, 8-hydroxypyrene-1,3,6-trisulfonic acid trisodium salt (HPTS), for the rapid and visual detection of PNA in aqueous media. The fluorescence quenching of HPTS caused by the presence of PNA was through non-covalent interactions. A good linear relationship between fluorescent intensity of HPTS at 512 nm was obtained in the range of 10-120 μmol/L. The detection limit (3σ) of this approach was 4. 6 μmol/L. The results showed that the method was suitable for rapid detection of PNA in real samples with good sensitivity, selectivity, anti-interference, low cost and easy operation.

Condition of p-nitroaniline Degrading Microbacterium sp. PNA8 and Its Degradation of p-nitroaniline / 微生物学通报

A bacterial strain capable of utilizing p-nitroaniline as sole carbon source to growth was isolated from sewage sludge. This strain was identified as Microbacterium sp. PNA8 based on its morphology, physiological, biochemical properties and 16S rRNA sequence analysis. Results indicated that the optimal temperature and pH for cell growth and for p-nitroaniline degradation was 30?C and 7.0. Strain PNA8 growth and p-nitroaniline degradation was considerably faster in the presence of yeast extract. Optimum conditions, in the culture medium added to 0.4 g/L yeast extract, 0.3 mmol/L p-nitroaniline degradation rate to 100% in 4 days.