Le Zhen
China Pharmaceutical University
Network
Latest external collaboration on country level. Dive into details by clicking on the dots.
Publication
Featured researches published by Le Zhen.
Organic Letters | 2015
Chao Lin; Le Zhen; Yong Cheng; Hong-Jin Du; Hui Zhao; Xiaoan Wen; Ling-Yi Kong; Qing-Long Xu; Hongbin Sun
Visible-light induced isoindole formation triggered an intermolecular Diels-Alder reaction with dienophiles such as acetylenedicarboxylate and maleimides in the presence of air. The reaction resulted in excellent diastereoselctivity and high yields under mild reaction conditions. This protocol provides an atom-economical, transition-metal-free (TM-free) and straightforward approach to structurally diverse bridged-ring heterocycles from easily accessible molecules.
Beilstein Journal of Organic Chemistry | 2014
Chun-Huan Jiang; Xiantao Lei; Le Zhen; Hong-Jin Du; Xiaoan Wen; Qing-Long Xu; Hongbin Sun
Summary Lewis acid-catalyzed redox-neutral amination of 2-(3-pyrroline-1-yl)benzaldehydes via intramolcular [1,5]-hydride shift/isomerization reaction has been realized, using the inherent reducing power of 3-pyrrolines. A series of N-arylpyrrole containing amines are obtained in high yields.
Bioorganic & Medicinal Chemistry Letters | 2011
Jun Xia; Jianfei Song; Le Zhen; Xiuling Zhang; Xiantao Lei; Lina Zheng; Qiujuan Wang; Hongbin Sun
A series of novel 2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3,3-diphenyl butyric acid derivatives were synthesized and evaluated for their antagonistic activity for endothelin-1-induced contraction in rabbit aorta. Within this series of compounds, 2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-cyano-3,3-diphenylpropionic acid (4) displays comparable potency with ambrisentan (1), and warrants further investigation.
Organic Letters | 2017
Le Zhen; Jiankun Wang; Qing-Long Xu; Hongbin Sun; Xiaoan Wen; Guangji Wang
A novel Ugi-type reaction triggered by 1,5-hydride shift has been established, giving access to N-arylprolinamides and related compounds in high atom economy and good yields. This is an example of a two starting material-three component reaction. The benzyl alcohol substrate 1 acts as a dual synthon, which upon treatment with a Brønsted acid affords iminium ion and water. Nucleophilic attack at the iminium ion by the third component isocyanide, followed by hydrolysis with the endogenic water, gives the Ugi-type reaction products. The reaction proceeds under mild conditions and is tolerable to a broad scope of substrates.
Journal of Chromatography B | 2018
Yilin Sun; Le Zhen; Ying Peng; Jiankun Wang; Fei Fei; Lixiang Aa; Wenjiao Jiang; Xue Pei; Li Lu; Jie Liu; Guangji Wang; Kun Hao
To improve bioavailability and provide resistance to deamination, an array of gemcitabine (dFdC) prodrugs carrying the acyl modifications has been successful in the optimization of pharmacokinetic properties of dFdC, but the reports about 4-N-carbobenzoxy-dFdC (Cbz-dFdC), a dFdC prodrug bearing alkyloxycarbonyl modification, are relatively rare. Notably, in vivo enzymatic hydrolysis was an absolutely essential factor for the activation of these prodrugs, which is correlated with the anti-tumor activity. Therefore, detailed metabolism studies of Cbz-dFdC should be carried out for a more authentic pharmacodynamic evaluation. In order to detect the pharmacokinetic characteristics of Cbz-dFdC, a selective, sensitive and accurate method for the simultaneous determination of Cbz-dFdC, along with dFdC and its major metabolite dFdU in rat plasma was developed and validated using UFLC-MS/MS techniques. Column was at 40 °C for separation using an eluent with acetonitrile and 0.1% formic acid, 1 mM ammonium formate at a flow rate of 0.2 mL/min. Detection was performed using ESI source in positive ion selected reaction monitoring mode by monitoring the following ion transitions m/z 398.1 → 202.2 (Cbz-dFdC), m/z 264.1 → 112.0 (dFdC), m/z 265.3 → 113.2 (dFdU) and m/z 246.1 → 112.0 (IS). Analytes were extracted by simple precipitation with acetonitrile containing internal standards followed by liquid-liquid extraction with ethyl acetate. The calibration curves of Cbz-dFdC, dFdC and dFdU were linear in the concentration range of 2 to 500 ng/mL, 2 to 500 ng/mL and 40 to 10,000 ng/mL, respectively. The assay ranges selected for the three analytes were appropriate and minimized the need for reanalysis. All the validation data, such as intra- and inter-day precision, accuracy, selectivity and stability, were within the required limits. In conclusion, the sensitive analytical assay was selective and accurate for the determination of rat plasma concentrations of Cbz-dFdC, dFdC and dFdU from a single LC-MS/MS analysis and well-suited to support pharmacokinetic studies.
Journal of Organic Chemistry | 2018
Jiankun Wang; Yilin Sun; Mu-Han Jiang; Tian-Yu Hu; Yong-Jie Zhao; Xin Li; Guangji Wang; Kun Hao; Le Zhen
A practical metal-free oxidative Ugi-type three-component assembly has been achieved efficiently, employing a tertiary-amine-derived iminium ion as an imine surrogate, N-hydroxyimide as an acid surrogate, and DEAD as an oxidant. This dual-surrogate Ugi variant proceeded with a broad substrate scope and desired functional group tolerance, leading to a wide range of N-alkyl- N-acyl aminophthalimide and N-alkyl- N-acylaminosuccinimide derivatives in good isolated yields.
Organic and Biomolecular Chemistry | 2014
Hong-Jin Du; Le Zhen; Xiaoan Wen; Qing-Long Xu; Hongbin Sun
Tetrahedron | 2015
Le Zhen; Chao Lin; Hong-Jin Du; Liang Dai; Xiaoan Wen; Qing-Long Xu; Hongbin Sun
European Journal of Organic Chemistry | 2017
Le Zhen; Liang Dai; Sheng-Qi Yu; Chao Lin; Hongbin Sun; Qing-Long Xu
Journal of Medicinal Chemistry | 2017
Le Zhen; Liang Dai; Xiaoan Wen; Lan Yao; Xiaoliang Jin; Xiao-Wen Yang; Wenfeng Zhao; Sheng-Qi Yu; Haoliang Yuan; Guangji Wang; Hongbin Sun