Selective synthesis of L ‐2‐18Ffluoro‐alpha‐methylphenylalanine via copper mediated 18F‐fluorination of (mesityl)(aryl)iodonium salt

L ‐2‐[18F]fluoro ‐alpha‐methylphenylalanine (2‐[18F]FAMP) is a promising amino acid tracer for positron emission tomography (PET) imaging, yet the low production yield of direct electrophilic radiofluorination with [18F]F2 necessitates further optimization of the radiolabeling process. This paper describes a 2 ‐step preparation method for L‐2‐[18F]fluoro ‐alpha‐methylphenylalanine (2‐[18F]FAMP) starting from [18F]fluoride.The (Mesityl)(L ‐alpha‐methylphenylalanine)‐2‐iodonium tetrafluoroborate precursors with various protecting groups were prepared. The copper‐mediated18F ‐fluorination of the iodonium salt precursors successfully produced 2‐[18F]FAMP. The highest radio chemical conversion of 57.6% was noted withN‐Piv‐protected (mesityl)(aryl)iodonium salt in the presence of 5 equivalent of Cu (OTf)2. Subsequent deprotection with 57% hydrogen iodide produced 2 ‐[18F]FAMP within 120 min in 21.4 ±11.7% overall radiochemical yield with>95% radiochemical purity and an enantiomeric excess>99%. The obtained 2 ‐[18F]FAMP showed comparable biodistribution profiles in normal mice with that of the carrier ‐added 2‐[18F]FAMP.These results indicate that usefulness of copper mediated18F ‐fluorination for the production of 2‐[18F]FAMP, which would facilitate clinical translation of the promising tumor specific amino acid tracer. Individual facilities could adopt either production method based on radioactivity demand and equipm...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - Category: Biochemistry Authors: Tags: RESEARCH ARTICLE Source Type: research

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Source: Advances in Experimental Medicine and Biology - Category: Research Tags: Adv Exp Med Biol Source Type: research
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Source: MICCAI International Conference on Medical Image Computing and Computer-Assisted Intervention - Category: Radiology Tags: Med Image Comput Comput Assist Interv Source Type: research
The objective of the study was to design, fabricate, and investigate the effectiveness of microneedle ocular patch (MOP) in delivering the model drug, pilocarpine HCl across the corneal membrane.Methods: MOP mimicked commercially available contact lens design elements having a diameter of 14.20 mm and a sagittal height of 3.85 mm with a convex curvature. The base of this patch contained an array of 25 pyramid-shaped microneedles measuring 521 ± 10 µm in length. Pilocarpine loaded MOP was prepared by micromolding technique using dissolvable polyvinyl alcohol and polyvinyl pyrrolidone...
Source: Drug Development and Industrial Pharmacy - Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research
In this study, mushroom residue was adding in lead-zinc slag to enhance the phytoremediation potential of P. fortunei, the effects of three treatments (lead-zinc slag, red soil, lead-zinc slag + 10% (m/m) mushroom residue) on the growth, physiology and microstructure of P. fortunei were determined. The results showed that the addition of mushroom residue increased the biomass, plant height and chlorophyll concentration of P. fortunei, indicating that the addition of mushroom residue can facilitate the growth of P. fortunei. Moreover, the proportions of oxalate-Pb forms and phosphate-Zn were do...
Source: Chemosphere - Category: Chemistry Authors: Tags: Chemosphere Source Type: research
This study aimed to investigate how a unilateral high-grade tear caused overdistension of LAM and whether tear positions affect the degree of distension. Methods A total of 209 women were screened by translabial ultrasonography. Then, 18 nulliparous women with an intact LAM and 26 postpartum women with unilateral levator ani defects were recruited. The anteroposterior diameter (AP), coronal diameter (LR), and hiatal area (HA) of the minimum levator hiatus were recorded and compared for assessing the distensibility. All 44 subjects underwent magnetic resonance imaging for the diagnosis of levator ani defect and detection...
Source: Female Pelvic Medicine and Reconstructive Surgery - Category: OBGYN Tags: Original Articles Source Type: research
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Source: ASAIO Journal - Category: Medical Devices Tags: Management of COVID-19 Patients Source Type: research
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Source: Biomed Res - Category: Research Authors: Tags: Biomed Res Int Source Type: research
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Source: Biomed Res - Category: Research Authors: Tags: Biomed Res Int Source Type: research
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Source: SafetyLit - Category: International Medicine & Public Health Tags: Risk Factor Prevalence, Injury Occurrence Source Type: news
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Source: Obesity Surgery - Category: Surgery Source Type: research
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