Metal‐Free Synthesis of Functional 1‐Substituted‐1,2,3‐Triazoles from Ethenesulfonyl Fluoride and Organic Azides
作者:Marie‐Claire Giel、Christopher J. Smedley、Emily R. R. Mackie、Taijie Guo、Jiajia Dong、Tatiana P. Soares da Costa、John E. Moses
DOI:10.1002/anie.201912728
日期:2020.1.13
scalable click-inspired protocol for the synthesis of 1-substituted-1,2,3-triazoles from organicazides and the bench stable acetylene surrogate ethenesulfonyl fluoride (ESF). The new transformation tolerates a wide selection of substrates and proceeds smoothly under metal-free conditions to give the products in excellent yield. Under controlled acidic conditions, the 1-substituted-1,2,3-triazole products
Preparation of Aryl Azides from Aromatic Amines in <i>N</i>-Methyl-2-Pyrrolidonium Bisulfate
作者:Abdol Reza Hajipour、Fatemeh Mohammadsaleh
DOI:10.1080/00304948.2011.613695
日期:2011.1.1
for azidation of aromatic compounds25 by a diazotization-azidation sequence. In the present work, we have developed an efficient and simple method for the diazotization and azidation of aromatic amines using the acidic ionic liquid N-methyl-2-pyrrolidonium bisulfate ([H-NMP]HSO4) as solvent and a novel proton source for the diazotization process at room temperature. The diazotization of various aryl
miRNA PROCESSING INHIBITOR EFFICACY ASSAYS AND SUBSTANCES
申请人:Arenz Christoph
公开号:US20090092980A1
公开(公告)日:2009-04-09
The invention relates to assays for assessing miRNA maturation effector (preferably: inhibitor) efficacy, and to substances useful for influencing, particularly for inhibiting, maturation of miRNA. According to the invention there is provided assay of miRNA processing inhibitor efficacy, comprising the steps of: a) providing a target miRNA precursor, b) providing a potential inhibitor of one or more processing steps of the target miRNA precursor, c) bringing together of the target miRNA precursor and the potential inhibitor under miRNA maturation conditions, and d) determining inhibition efficiency. The assay of the present invention allows for a very fast and easy assessment of the efficacy of a potential inhibitor in inhibiting processing of a miRNA precursor into miRNA.
Chemistry of Tetradentate [
<i>C</i>
,
<i>N : C</i>
,
<i>N</i>
] Iminophosphorane Palladacycles: Preparation, Reactivity and Theoretical Calculations
作者:Paula Munín‐Cruz、Francisco Reigosa、Marcos Rúa‐Sueiro、Juan M. Ortigueira、M. Teresa Pereira、José M. Vila
DOI:10.1002/open.202000253
日期:2020.11
A theoretical and experimental study of tetradentate [C,N : C,N] iminophosphorane palladacycles was carried out for the purpose of elucidating their behavior as compared to the parent Schiff base analogues to determine the prospect of encountering new A‐frame structures for the iminophosphorane derivatives. The DFT calculations were in agreement with the experimental results regarding the performance
对四齿 [C,N : C,N] 亚氨基正膦钯环进行了理论和实验研究,目的是阐明其与母体席夫碱类似物相比的行为,以确定亚氨基正膦新 A 框架结构的前景衍生物。DFT 计算与这些配体性能的实验结果一致。对相关双核物种的化学有了新的见解。
Harnessing pyrrolidine iminosugars into dimeric structures for the rapid discovery of divalent glycosidase inhibitors
作者:Ana T. Carmona、Sebastián Carrión-Jiménez、Valeria Pingitore、Elena Moreno-Clavijo、Inmaculada Robina、Antonio J. Moreno-Vargas
DOI:10.1016/j.ejmech.2018.04.008
日期:2018.5
libraries (1a-l, 1a'-l' and 2a-l) of dimeric iminosugars through CuAAC reaction between three different alkynyl pyrrolidines and a set of diazides was carried out. The resulting crude dimers were screened in situ against two α-fucosidases (libraries 1a-l and 1a'-l') and one β-galactosidase (2a-l). This method is pioneer in the search of divalent glycosidase inhibitors. It has allowed the rapid identification