Immobilization of a chiral dirhodium catalyst on SBA-15 via click-chemistry: Application in the asymmetric cyclopropanation of 3-diazooxindole with aryl alkenes

2021 ◽  
Vol 52 ◽  
pp. 101682
Author(s):  
Zhenzhong Li ◽  
Lorenz Rösler ◽  
Till Wissel ◽  
Hergen Breitzke ◽  
Torsten Gutmann ◽  
...  
Author(s):  
Qinheng Zheng ◽  
Hongtao Xu ◽  
Hua Wang ◽  
Wen-Ge Han Du ◽  
Nan Wang ◽  
...  

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).


2018 ◽  
Author(s):  
Marc Montesinos-Magraner ◽  
Matteo Costantini ◽  
Rodrigo Ramirez-Contreras ◽  
Michael E. Muratore ◽  
Magnus J. Johansson ◽  
...  

Asymmetric cyclopropane synthesis currently requires bespoke strategies, methods, substrates and reagents, even when targeting similar compounds. This limits the speed and chemical space available for discovery campaigns. Here we introduce a practical and versatile diazocompound, and we demonstrate its performance in the first unified asymmetric synthesis of functionalized cyclopropanes. We found that the redox-active leaving group in this reagent enhances the reactivity and selectivity of geminal carbene transfer. This effect enabled the asymmetric cyclopropanation of a wide range of olefins including unactivated aliphatic alkenes, enabling the 3-step total synthesis of (–)-dictyopterene A. This unified synthetic approach delivers high enantioselectivities that are independent of the stereoelectronic properties of the functional groups transferred. Our results demonstrate that orthogonally-differentiated diazocompounds are viable and advantageous equivalents of single-carbon chirons<i>.</i>


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

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

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

Author(s):  
Dace Cīrule ◽  
Kristers Ozols ◽  
Irina Novosjolova ◽  
Māris Turks ◽  
Ērika Bizdēna

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