A 1,4-Diphenyl-1,2,3-Triazole-Based β-Turn Mimic Constructed by Click Chemistry

2012 ◽  
Vol 77 (9) ◽  
pp. 4261-4270 ◽  
Author(s):  
Chun-Fang Wu ◽  
Xin Zhao ◽  
Wen-Xian Lan ◽  
Chunyang Cao ◽  
Jin-Tao Liu ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Turn Mimic

Click Chemistry Expedited Radiosynthesis: Sulfur [18F]fluoride Exchange of Aryl Fluorosulfates

2019 ◽  
Author(s):  
Qinheng Zheng ◽  
Hongtao Xu ◽  
Hua Wang ◽  
Wen-Ge Han Du ◽  
Nan Wang ◽  
...  
Keyword(s):  
Click Chemistry ◽  
High Performance ◽  
Isotopic Exchange ◽  
Tumor Imaging ◽  
Radiochemical Yield ◽  
Exchange Method ◽  
Molar Activity ◽  
Positron Emission ◽  
Sulfur Fluoride

The lack of simple, efficient [<sup>18</sup>F]fluorination processes and new target-specific organofluorine probes remains the major challenge of fluorine-18-based positron emission tomography (PET). We report here a fast isotopic exchange method for the radiosynthesis of aryl [<sup>18</sup>F]fluorosulfate based PET agents enabled by the emerging sulfur fluoride exchange (SuFEx) click chemistry. The method has been applied to the fully-automated <sup>18</sup>F-radiolabeling of twenty-five structurally diverse aryl fluorosulfates with excellent radiochemical yield (83–100%) and high molar activity (up to 281 GBq µmol<sup>–1</sup>) at room temperature in 30 seconds. The purification of radiotracers requires no time-consuming high-performance liquid chromatography (HPLC), but rather a simple cartridge filtration. The utility of aryl [<sup>18</sup>F]fluorosulfate is demonstrated by the <i>in vivo</i> tumor imaging by targeting poly(ADP-ribose) polymerase 1 (PARP1).

Use of Click-Chemistry in the Development of Peptidomimetic Enzyme Inhibitors

2014 ◽  
Vol 21 (13) ◽  
pp. 1467-1477 ◽  
Author(s):  
P. Fabbrizzi ◽  
G. Menchi ◽  
A. Guarna ◽  
A. Trabocchi
Keyword(s):  
Click Chemistry ◽  
Enzyme Inhibitors

Synthesis of Porphyrin, Chlorin and Phthalocyanine Derivatives by Azide-Alkyne Click Chemistry

2015 ◽  
Vol 22 (28) ◽  
pp. 3217-3254 ◽  
Author(s):  
Samir Acherar ◽  
Ludovic Colombeau ◽  
Celine Frochot ◽  
Regis Vanderesse
Keyword(s):  
Click Chemistry

Click Chemistry, A Potent Tool in Medicinal Sciences

2015 ◽  
Vol 22 (17) ◽  
pp. 2022-2050 ◽  
Author(s):  
F. Musumeci ◽  
S. Schenone ◽  
A. Desogus ◽  
E. Nieddu ◽  
D. Deodato ◽  
...  
Keyword(s):  
Click Chemistry

A synthetic route to 2,6-bis-triazolyl purine deoxynucleosides via click chemistry

2014 ◽  
Author(s):  
Dace Cīrule ◽  
Kristers Ozols ◽  
Irina Novosjolova ◽  
Māris Turks ◽  
Ērika Bizdēna
Keyword(s):  
Click Chemistry ◽  
Synthetic Route
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