1. Imidazole Hydrochloride Promoted Synthesis of Nitriles from Aldehydes
Yin Wang, Xuetong Wang, Yanwu Li, Xiuyu Zhang, Lingli Li, Tingshu He, Jianyong Yuan, Suqin Shang Curr Org Synth. 2022;19(8):923-929. doi: 10.2174/1570179419666220509143654.
Background and objective: As a key pharmacophore, the cyano group widely exists in a variety of biologically active compounds. Besides, nitriles are also valuable intermediates for many common functional groups. In this current work, a new synthesis strategy was developed to obtain nitriles from aldehydes. Methods: Using commercially available aldehydes as raw materials, and hydroxylamine and hydrochloride as nitrogen sources, the corresponding nitrile compounds were successfully synthesized by the one-pot method through the promotion of imidazole hydrochloride. And it was characterized by 1H NMR, 13C NMR, and mass spectrometry. Results: Various reaction conditions were applied in order to find an optimum and convenient procedure for the formation of nitriles. The highest yields (95%) were achieved using sulfolane as a solvent, and imidazole hydrochloride as a promoter. Conclusion: In conclusion, we developed a new synthetic method for nitrile compounds from aldehydes. Twenty seven examples of functionalized nitrile compounds have been synthesized in good to excellent yields. This methodology features that an environmentally benign imidazole hydrochloride replaces transition metal catalysts and oxidants required in conventional strategies to convert aldehydes into nitriles with good functional group tolerability. Further exploration of imidazole hydrochloride is ongoing in our laboratory.
2. Efficacy and safety of terbinafine hydrochloride spray and 3% boric acid alcohol ear drops in otomycosis
Shuai Xu, Jianfeng Li, Ling Ding, Kun Gao, Fengyang Xie, Jie Han, Xuanchen Zhou Acta Otolaryngol. 2020 Apr;140(4):302-306. doi: 10.1080/00016489.2020.1712474. Epub 2020 Feb 5.
Background: Although otomycosis is a disease spread throughout the world, there are only a few of studies about it.Objective: We aimed to evaluate the clinical efficacy of terbinafine hydrochloride spray (THS) in combination with 3% boric acid alcohol (3% BAA) ear drops compared to 3% BAA ear drops in otomycosis.Methods: This was a randomised, parallel-group, double-blind study involving 320 patients of both sexes aged 18 years or older.Results: The clinical cure rate was higher (p = .01) with THS in combination with 3% BAA ear drops than with 3% BAA ear drops alone. The change of mean total symptom score was significant with THS in combination with 3% BAA ear drops (p = .035). No differences were found in the percentage of patients reporting resolution of otalgia between patients receiving THS in combination with 3% BAA ear drops and those receiving only 3% BAA ear drops. Resolution rates of pruritus, otorrhea, aural fullness, tinnitus and hypoacusis (p = .005, p = .004, p = .002, p = .001, p = .004, respectively) was higher with THS in combination with 3% BAA ear drops, as was eradication (p = .001). There were seven mild adverse events, three with the THS in combination with 3% BAA ear drops (not related to the treatment) and four when 3% BAA was administered alone (not related to the treatment).Conclusions: THS in combination with 3% BAA ear drops is a more effective treatment for otomycosis than 3% BAA ear drops alone. The THS in combination with 3% BAA ear drops also has an excellent safety profile.Significance: To provides a safe and effective method for treating otomycosis.
3. Visible Light Response Photocatalytic Performance of Z-Scheme Ag3PO4/GO/UiO-66-NH2 Photocatalysts for the Levofloxacin Hydrochloride
Pengfei Zhu, Jinru Lin, Lisi Xie, Ming Duan, Dandan Chen, Dan Luo, Yongting Wu Langmuir. 2021 Nov 16;37(45):13309-13321. doi: 10.1021/acs.langmuir.1c01901. Epub 2021 Nov 7.
A Ag3PO4/GO/UiO-66-NH2(AGU) composite photocatalyst was prepared by an ultrasonic-assisted in situ precipitation method. The optical property, structure, composition, and morphology of photocatalysts were investigated using UV-vis diffuse reflectance spectroscopy, photoluminescence spectroscopy, electrochemical impedance spectroscopy, X-ray diffraction, X-ray photoelectron spectroscopy, scanning electron microscopy, energy-dispersive spectrometry, transmission electron microscopy, Fourier transform infrared spectroscopy, and charge flow tracking by photodeposition of Pt and PbO2 nanoparticles. In comparison with Ag3PO4 and Ag3PO4/UiO-66-NH2(AU), the AGU composite photocatalyst showed heightened photocatalytic performance for the degradation of levofloxacin hydrochloride (LVF). The AGU photocatalyst (dosage: 0.8 g/L) with 1% mass content of graphene oxide (GO), the mass ratio of Ag3PO4 and UiO-66-NH2(U66N) reached 2:1, showed the highest photodegradation rate of 94.97% for 25 mg/L LVF after 60 min of visible light irradiation at pH = 6. The formation of a heterojunction and the addition of GO synergistically promote faster separation of electron-hole pairs, retain more active substances, and enhance the performance of the photocatalyst. Furthermore, the mechanism of the Z-scheme of the AGU composite photocatalytic is proposed.
