scholarly journals One-pot and one-step automated radio-synthesis of [18F]AlF-FAPI-74 using a multi purpose synthesizer: a proof-of-concept experiment

2021 ◽  
Vol 6 (1) ◽  
Author(s):  
Sadahiro Naka ◽  
Tadashi Watabe ◽  
Thomas Lindner ◽  
Jens Cardinale ◽  
Kenta Kurimoto ◽  
...  
Keyword(s):  
Recovery Rate ◽  
Radiochemical Purity ◽  
Synthesis Method ◽  
Precursor Solution ◽  
Sodium Ascorbate ◽  
Automated Synthesis ◽  
One Pot ◽  
High Accumulation ◽  
One Step ◽  
Phosphate Buffered Saline

Abstract Background Fibroblast activation protein (FAP) is overexpressed in the stroma of many types of cancer. [18F]AlF-FAPI-74 is a positron emission tomography tracer with high selectivity for FAP, which has already shown high accumulation within human tumors in clinical studies. However, [18F]AlF-FAPI-74 radiosynthesis has not been optimized using an automated synthesizer. Herein, we report a one-pot and one-step automated radiosynthesis method using a multi purpose synthesizer. Results Radiosynthesis of [18F]AlF-FAPI-74 was performed using a cassette-type multi purpose synthesizer CFN-MPS200. After the recovery rate of trapped [18F]fluoride onto the anion-exchange cartridge using a small amount of eluent was investigated manually, a dedicated [18F]AlF-FAPI-74 synthesis cassette and synthesis program for one-pot and one-step fluorination was developed. The solutions for the formulation of [18F]AlF-FAPI-74 synthesized using this were evaluated to obtain stable radiochemical purity. The recovery rate of [18F]fluoride with only 300 µL of eluent ranged 90 ± 9% by introduction from the male side and elution from the female side of the cartridge. In automated synthesis, the eluted [18F]fluoride and precursor solution containing aluminum chloride were mixed; then, fluorination was performed in a one-pot and one-step process at room temperature for 5 min, followed by 15 min at 95 °C. As a result, the radioactivity of [18F]AlF-FAPI-74 was 11.3 ± 1.1 GBq at the end of synthesis from 32 to 40 GBq of [18F]fluoride, and its radiochemical yield was 37 ± 4% (n = 10). The radiochemical purity at the end of the synthesis was ≥ 97% for all formulation solutions. When the diluent was saline, the radiochemical purity markedly decreased after 4 h of synthesis. In contrast, with phosphate-buffered saline (pH 7.4) or 10 mM phosphate-buffered saline (pH 6.7) containing 100 mg of sodium ascorbate, the radiochemical purity was stable at 97%. Non-radioactive AlF-FAPI-74 and total impurities, including non-radioactive AlF-FAPI-74, were 0.3 ± 0.1 µg/mL and 2.8 ± 0.6 µg/mL. Ethanol concentration and residual DMSO were 5.5 ± 0.2% and 21 ± 6 ppm, respectively. Conclusions We established a one-pot one-step automated synthesis method using a CFN-MPS200 synthesizer that provided high radioactivity and stable radiochemical purity for possible clinical applications.

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.

One-step synthesis of poly(ethyleneglycol dimethacrylate)-microspheres-supported nano-Au catalyst in methanol–water solution under γ-ray radiation

RSC Advances ◽  
2016 ◽  
Vol 6 (61) ◽  
pp. 55878-55883 ◽  
Author(s):  
Jinxing Chen ◽  
Feng Chen ◽  
Yiyao Wang ◽  
Mozhen Wang ◽  
Qichao Wu ◽  
...  
Keyword(s):  
Radiation Effect ◽  
Water Solution ◽  
Synthesis Method ◽  
Au Catalyst ◽  
One Pot ◽  
System P ◽  
One Step ◽  
Γ Ray

Highly-crosslinked poly(ethyleneglycol dimethacrylate) (PEGDMA) microspheres supported nano-Au catalyst (PEGDMA@AuNP) was first prepared through a one-step synthesis method, taking advantage of the γ-ray radiation effect on a simple one-pot system.

scholarly journals Robust and Facile Automated Radiosynthesis of [18F]FSPG on the GE FASTlab

2021 ◽  
Author(s):  
Richard Edwards ◽  
Hannah E. Greenwood ◽  
Graeme McRobbie ◽  
Imtiaz Khan ◽  
Timothy H. Witney
Keyword(s):  
Large Scale ◽  
Radiochemical Purity ◽  
Radiochemical Yield ◽  
Automated Synthesis ◽  
Molar Activity ◽  
Positron Emission ◽  
Optimized Protocol ◽  
Cancer Types ◽  
Automated Procedures ◽  
Phosphate Buffered Saline

Abstract Purpose (S)-4-(3-18F-Fluoropropyl)-ʟ-Glutamic Acid ([18F]FSPG) is a radiolabeled non-natural amino acid that is used for positron emission tomography (PET) imaging of the glutamate/cystine antiporter, system xC-, whose expression is upregulated in many cancer types. To increase the clinical adoption of this radiotracer, reliable and facile automated procedures for [18F]FSPG production are required. Here, we report a cassette-based method to produce [18F]FSPG at high radioactivity concentrations from low amounts of starting activity. Procedures An automated synthesis and purification of [18F]FSPG was developed using the GE FASTlab. Optimization of the reaction conditions and automated manipulations were performed by measuring the isolated radiochemical yield of [18F]FSPG and by assessing radiochemical purity using radio-HPLC. Purification of [18F]FSPG was conducted by trapping and washing of the radiotracer on Oasis MCX SPE cartridges, followed by a reverse elution of [18F]FSPG in phosphate-buffered saline. Subsequently, the [18F]FSPG obtained from the optimized process was used to image an animal model of non-small cell lung cancer. Results The optimized protocol produced [18F]FSPG in 38.4 ± 2.6 % radiochemical yield and >96 % radiochemical purity with a molar activity of 11.1 ± 7.7 GBq/μmol. Small alterations, including the implementation of a reverse elution and an altered Hypercarb cartridge, led to significant improvements in radiotracer concentration from <10 MBq/ml to >100 MBq/ml. The improved radiotracer concentration allowed for the imaging of up to 20 mice, starting with just 1.5 GBq of [18F]Fluoride. Conclusions We have developed a robust and facile method for [18F]FSPG radiosynthesis in high radiotracer concentration, radiochemical yield, and radiochemical purity. This cassette-based method enabled the production of [18F]FSPG at radioactive concentrations sufficient to facilitate large-scale preclinical experiments with a single prep of starting activity. The use of a cassette-based radiosynthesis on an automated synthesis module routinely used for clinical production makes the method amenable to rapid and widespread clinical translation.

scholarly journals One-pot synthesis of NiAl–CO3 LDH anti-corrosion coatings from CO2-saturated precursors

RSC Advances ◽  
2015 ◽  
Vol 5 (37) ◽  
pp. 29552-29557 ◽  
Author(s):  
Yi Liu ◽  
Tongwen Yu ◽  
Rui Cai ◽  
Yanshuo Li ◽  
Weishen Yang ◽  
...  
Keyword(s):  
Mechanical Stability ◽  
Precursor Solution ◽  
One Pot ◽  
One Pot Synthesis ◽  
One Step

In this study, well-intergrown NiAl–CO3 LDH films with excellent anti-corrosive capacity, considerable long-term corrosion durability as well as strong mechanical stability are prepared from CO2-saturated precursor solution in one step.

A Study on the Rearrangement of Dialkyl 1-Aryl-1-hydroxymethylphosphonates to Benzyl Phosphates

2020 ◽  
Vol 24 (4) ◽  
pp. 465-471 ◽  
Author(s):  
Zita Rádai ◽  
Réka Szabó ◽  
Áron Szigetvári ◽  
Nóra Zsuzsa Kiss ◽  
Zoltán Mucsi ◽  
...  
Keyword(s):  
Quantum Chemical ◽  
Room Temperature ◽  
Phase Transfer ◽  
One Pot ◽  
Substrate Dependence ◽  
Triethylbenzylammonium Chloride ◽  
One Step ◽  
The Pudovik Reaction ◽  
The One ◽  
Solid Liquid

The phospha-Brook rearrangement of dialkyl 1-aryl-1-hydroxymethylphosphonates (HPs) to the corresponding benzyl phosphates (BPs) has been elaborated under solid-liquid phase transfer catalytic conditions. The best procedure involved the use of triethylbenzylammonium chloride as the catalyst and Cs2CO3 as the base in acetonitrile as the solvent at room temperature. The substrate dependence of the rearrangement has been studied, and the mechanism of the transformation under discussion was explored by quantum chemical calculations. The key intermediate is an oxaphosphirane. The one-pot version starting with the Pudovik reaction has also been developed. The conditions of this tandem transformation were the same, as those for the one-step HP→BP conversion.

A Simple Synthesis of the Anticancer Drug Altretamine

2020 ◽  
Vol 17 (8) ◽  
pp. 628-630
Author(s):  
Vu Binh Duong ◽  
Pham Van Hien ◽  
Tran Thai Ngoc ◽  
Phan Dinh Chau ◽  
Tran Khac Vu
Keyword(s):  
Aqueous Solution ◽  
Anticancer Drug ◽  
Potassium Hydroxide ◽  
Large Scale ◽  
Synthesis Method ◽  
Practical Method ◽  
Cyanuric Chloride ◽  
Simple Synthesis ◽  
High Yield ◽  
One Step

A simple and practical method for the synthesis on a large scale of altretamine (1), a wellknown antitumor drug, has been successfully developed. The synthesis method involves the conversion of cyanuric chloride (2) into altretamine (1) by dimethylamination of 2 with an aqueous solution of 40% dimethylamine and potassium hydroxide in 1, -dioxan 4in one step to give altretamine (1) in high yield.

Thermally stable amine-functionalized silica sorbents using one-pot synthesis method for CO2 capture at low temperature

2020 ◽  
Vol 37 (12) ◽  
pp. 2317-2325
Author(s):  
Seong Bin Jo ◽  
Ho Jin Chae ◽  
Tae Young Kim ◽  
Jeom-In Baek ◽  
Dhanusuraman Ragupathy ◽  
...  
Keyword(s):  
Low Temperature ◽  
Co2 Capture ◽  
Synthesis Method ◽  
Functionalized Silica ◽  
Thermally Stable ◽  
One Pot ◽  
One Pot Synthesis ◽  
Amine Functionalized

scholarly journals One-step synthesis of nitrogen-grafted copper-gallic acid for enhanced methylene blue removal

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Shella Permatasari Santoso ◽  
Vania Bundjaja ◽  
Artik Elisa Angkawijaya ◽  
Chintya Gunarto ◽  
Alchris Woo Go ◽  
...  
Keyword(s):  
Methylene Blue ◽  
Adsorption Capacity ◽  
Gallic Acid ◽  
Synthesis Method ◽  
Molar Ratio ◽  
X Ray Diffraction ◽  
Temperature Dependent ◽  
One Step ◽  
Detailed Assessment ◽  
Higher Temperature

AbstractNitrogen-grafting through the addition of glycine (Gly) was performed on a metal- phenolic network (MPN) of copper (Cu2+) and gallic acid (GA) to increase its adsorption capacity. Herein, we reported a one-step synthesis method of MPN, which was developed according to the metal–ligand complexation principle. The nitrogen grafted CuGA (Ng-CuGA) MPN was obtained by reacting Cu2+, GA, and Gly in an aqueous solution at a molar ratio of 1:1:1 and a pH of 8. Several physicochemical measurements, such as Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), N2 sorption, X-ray diffraction (XRD), and thermal gravimetry analysis (TGA), were done on Ng-CuGA to elucidate its characteristics. The analysis revealed that the Ng-CuGA has non-uniform spherical shaped morphology with a pore volume of 0.56 cc/g, a pore size of 23.25 nm, and thermal stability up to 205 °C. The applicational potential of the Ng-CuGA was determined based on its adsorption capacity against methylene blue (MB). The Ng-CuGA was able to adsorb 190.81 mg MB per g adsorbent at a pH of 6 and temperature of 30 °C, which is 1.53 times higher than the non-grafted CuGA. Detailed assessment of Ng-CuGA adsorption properties revealed their pH- and temperature-dependent nature. The adsorption capacity and affinity were found to decrease at a higher temperature, demonstrating the exothermic adsorption behavior.

scholarly journals Efficient Adsorption of Methylene Blue by Porous Biochar Derived from Soybean Dreg Using a One-Pot Synthesis Method

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 661
Author(s):  
Zhiwei Ying ◽  
Xinwei Chen ◽  
He Li ◽  
Xinqi Liu ◽  
Chi Zhang ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Methylene Blue ◽  
Photoelectron Spectroscopy ◽  
Synthesis Method ◽  
Urban Pollution ◽  
Maximum Adsorption Capacity ◽  
One Pot ◽  
Average Pore ◽  
X Ray ◽  
Isotherm Equation

Soybean dreg is a by-product of soybean products production, with a large consumption in China. Low utilization value leads to random discarding, which is one of the important sources of urban pollution. In this work, porous biochar was synthesized using a one-pot method and potassium bicarbonate (KHCO3) with low-cost soybean dreg (SD) powder as the carbon precursor to investigating the adsorption of methylene blue (MB). The prepared samples were characterized with scanning electron microscopy (SEM), transmission electron microscopy (TEM), elemental analyzer (EA), Brunauer-Emmett-Teller (BET), X-ray diffractometer (XRD), Raman spectroscopy (Raman), Fourier transform infrared spectrometer (FTIR), and X-ray photoelectron spectroscopy (XPS). The obtained SDB-K-3 showed a high specific surface area of 1620 m2 g−1, a large pore volume of 0.7509 cm3 g−1, and an average pore diameter of 1.859 nm. The results indicated that the maximum adsorption capacity of SDB-K-3 to MB could reach 1273.51 mg g−1 at 318 K. The kinetic data were most consistent with the pseudo-second-order model and the adsorption behavior was more suitable for the Langmuir isotherm equation. This study demonstrated that the porous biochar adsorbent can be prepared from soybean dreg by high value utilization, and it could hold significant potential for dye wastewater treatment in the future.

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