scholarly journals One-Step Synthesis of N-Succinimidyl-4-[18F]Fluorobenzoate ([18F]SFB)

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3436 ◽  
Author(s):  
Ida Nymann Petersen ◽  
Jacob Madsen ◽  
Christian Bernard Matthijs Poulie ◽  
Andreas Kjær ◽  
Matthias Manfred Herth
Keyword(s):  
Solid Phase Extraction ◽  
Total Synthesis ◽  
Radiochemical Purity ◽  
Solid Phase ◽  
Phase Extraction ◽  
One Pot ◽  
Synthesis Time ◽  
Synthesis Route ◽  
One Step

Herein, we present a one-step labeling procedure of N-succinimidyl-4-[18F]-fluorobenzoate ([18F]SFB) starting from spirocyclic iodonium ylide precursors. Precursor syntheses succeeded via a simple one-pot, two-step synthesis sequence, in yields of approximately 25%. Subsequent 18F-nucleophilic aromatic labeling was performed, and radiochemical incorporations (RCCs) from 5–35% were observed. Purification could be carried out using HPLC and subsequent solid phase extraction. Radiochemical purity (RCP) of >95% was determined. The total synthesis time, including purification and formulation, was no longer than 60 min. In comparison to the established 3-step synthesis route of [18F]SFB, this one-step approach avoids formation of volatile radioactive side-products and simplifies automatization.

scholarly journals A Purification Method of 18F-FP-(+)-DTBZ via Solid-Phase Extraction With Combined Cartridges

2021 ◽  
Vol 8 ◽  
Author(s):  
Yuyin Dai ◽  
Ri Sa ◽  
Feng Guan ◽  
Qi Wang ◽  
Yinghua Li ◽  
...  
Keyword(s):  
Solid Phase Extraction ◽  
Healthy Volunteers ◽  
Radiochemical Purity ◽  
Solid Phase ◽  
High Yield ◽  
Phase Extraction ◽  
Purification Method ◽  
Synthesis Time ◽  
Combined Use ◽  
Spe Purification

Background: To optimize [18F] 9-fluoropropyl-(+)-dihydrotetrabenazine (18F-FP-(+)-DTBZ) purification via solid-phase extraction (SPE) with combined cartridges to facilitate its widespread clinical application.Methods: A modified SPE purification method, employing Sep-Pak PS-2 and Sep-Pak C18 cartridges, was used for the preparation of 18F-FP-(+)-DTBZ. This method was compared to the purification method of high-pressure liquid chromatography (HPLC) and SPE with one cartridge, following quality control test and positron emission tomography (PET) imaging in healthy volunteers and patients with parkinsn's disease (PD).Results: A SPE purification method integrating Sep-Pak PS-2 and Sep-Pak C18 cartridges was implemented successfully. The retention time of 18F-FP-(+)-DTBZ purified by HPLC, SPE with Sep-Pak PS-2, SPE with Sep-Pak C18, and SPE with combined use of Sep-Pak PS-2 and Sep-Pak C18 cartridges was 8.7, 8.8, 8.7, and 8.9 min, respectively. Fewest impurity peak was detected in 18F-FP-(+)-DTBZ purified by the SPE with combined use of Sep-Pak PS-2 and Sep-Pak C18 cartridges. This modified SPE purification method provided a satisfactory radiochemical yield of 29 ± 1.8% with radiochemical purity >99% and shortened synthesis time to 27 min. The brain uptake of 18F-FP-(+)-DTBZ purified by the modified SPE was comparable to that purified by HPLC in both healthy volunteers and PD patients.Conclusions: A SPE method integrating Sep-Pak PS-2 and Sep-Pak C18 cartridges for purification of 18F-FP-(+)-DTBZ may be highly suited to automatic synthesis for routine clinical applications, as it provides excellent radiochemical purity, high yield as well as operational simplicity.

Radiosynthesis of a Novel PET Fluoronicotinamide for Melanoma Tumour PET Imaging; [18F]MEL050

2011 ◽  
Vol 64 (7) ◽  
pp. 873 ◽  
Author(s):  
Ivan Greguric ◽  
Stephen Taylor ◽  
Tien Pham ◽  
Naomi Wyatt ◽  
Cathy D. Jiang ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Large Scale ◽  
Radiochemical Purity ◽  
Specific Activity ◽  
Phase 1 ◽  
Radiochemical Yield ◽  
Synthesis Time ◽  
Clinical Phase ◽  
One Step ◽  
No Carrier Added

[18F]6-Fluoro-N-[2-(diethylamino)ethyl]nicotinamide [18F]MEL050 is a novel nicotinamide-based radiotracer, designed to target random metastatic dissemination of melanoma tumours by targeting melanin. Preclinical studies suggest that [18F]MEL050 has an excellent potential to improve diagnosis and staging of melanoma. Here we report the radiochemical optimization conditions of [18F]MEL050 and its large scale automated synthesis using a GE FXFN automated radiosynthesis module for clinical, phase-1 investigation. [18F]MEL050 was prepared via a one-step synthesis using no-carrier added K[18F]F-Krytpofix® 222 (DMSO, 170°C, 5 min) followed by HPLC purification. Using 6-chloro-N-[2-(diethylamino)ethyl]nicotinamide as precursor, [18F]MEL050 was obtained in 40–46% radiochemical yield (non-decay corrected), in greater than 99.9% radiochemical purity and specific activity ranging from 240 to 325 GBq μmol–1. Total synthesis time including formulation was 40 min and [18F]MEL050 was stable (99.8%) in PBS for 6 h.

scholarly journals One-Step Solid-Phase Extraction Procedure for F2-Isoprostanes

2001 ◽  
Vol 47 (7) ◽  
pp. 1306-1308 ◽  
Author(s):  
Zheng Zhao ◽  
N Magus Hjelm ◽  
Christopher W K Lam ◽  
Chung S Ho
Keyword(s):  
Solid Phase Extraction ◽  
Solid Phase ◽  
Extraction Procedure ◽  
Phase Extraction ◽  
Solid Phase Extraction Procedure ◽  
One Step

One-step fabrication of hydrophilic MIL-68(Al)/Chitosan-coated melamine sponge for vortex-assisted solid-phase extraction of parabens in water samples

Talanta ◽  
2021 ◽  
Vol 224 ◽  
pp. 121799
Author(s):  
Yanxiao Jiang ◽  
Bo Zhang ◽  
Jingkang Li ◽  
Ying Sun ◽  
Xinghua Wang ◽  
...  
Keyword(s):  
Solid Phase Extraction ◽  
Water Samples ◽  
Solid Phase ◽  
Phase Extraction ◽  
One Step
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