[18F]Fluoride recovery via gaseous [18F]HF

Acidification of target water with H₂SO₄ in a specially constructed glassy carbon/polyethylene apparatus allowed for recovery of up to 82% of [¹⁸F]fluoride as [¹⁸F]HF gas. The [¹⁸F]HF distillate was found to be acid‐free but moist; when passed through a solution of ^tBuPh₂SiOTf, it yielded [¹⁸F]^tBuPh₂SiF. The multivariate design of experiment showed that the key to high yield of [¹⁸F]HF was the efficient degassing of the reaction mixture.     

How to increase the reactivity of [18F]fluoroethyl bromide: [18F]fluoroethylation of amine,phenol and amide functional groups with [18F]FEtBr, [18F]FEtBr/NaI and [18F]FEtOTf

[¹⁸F]Fluoroethyl bromide ([¹⁸F]FEtBr) is a useful synthetic precursor to synthesize ¹⁸F‐labeled compounds. However, the lower reactivity of [¹⁸F]FEtBr with amine, phenol and amide functional groups than that of [¹¹C]CH₃I partly limits its wide application in the synthesis of [¹⁸F]fluoroethylated compounds. The aim of this study was to increase the reactivity of [¹⁸F]FEtBr with various nucleophilic substrates for PET tracers containing amine, phenol and amide moieties. The present strategies included (1) adding NaI into the reaction mixture of [¹⁸F]FEtBr and substrate, where [¹⁸F]FEtI is reversibly formed and becomes more reactive; (2) converting [¹⁸F]FEtBr into much more reactive [¹⁸F]FEtOTf, similar to conversion of [¹¹C]CH₃I into [¹¹C]CH₃OTf. By these efforts, the [¹⁸F]fluoroethylation efficiency of various substrates containing amine, phenol and amide groups with [¹⁸F]FEtBr/NaI and [¹⁸F]FEtOTf was significantly improved, compared with the corresponding reaction efficiency with [¹⁸F]FEtBr. Copyright © 2003 John Wiley & Sons, Ltd.     

Development of a new precursor‐minimizing base control method and its application for the automated synthesis and SPE purification of [18F]fluoromisonidazole ([18F]FMISO)

Bases such as potassium carbonate and potassium bicarbonate (KHCO₃) are essential for the elution of trapped [¹⁸F]fluoride from ion exchange cartridges and for the prevention of [¹⁸F]fluoride adsorption on the silica glass vial during the preparation of radiopharmaceuticals for positron emission tomography imaging. However, these bases promote the chemical decomposition of precursor compounds and the creation of unwanted organic impurities. Thus, the goal of the current study was to develop a new method for synthesizing [¹⁸F]fluoride‐labeled radiopharmaceuticals (e.g., [¹⁸F]fluoromisonizadole ([¹⁸F]FMISO)) that permits the fine control of base concentrations while minimizing adverse events. Non‐decay‐corrected radiochemical yields of 25.1 ± 5.0% and 13.3 ± 5.1% (n = 3) were achieved after solid‐phase extraction purification using automatic synthesis with GE TRACERlab MX and KHCO₃ at concentrations of 14.1 and 33.0 µmol, respectively, and 1 mg of precursor (1‐(2′‐nitro‐1′‐imidazolyl)‐2‐O‐tetra‐hydropyranyl‐3‐O‐toluenesulfonyl propanediol (NITTP)). The newly developed synthesis protocol with fine base control and low precursor content permits high radiochemical yields with minimal impurities. Copyright © 2013 John Wiley & Sons, Ltd.     

A simple and rapid automated radiosynthesis of [18F]fluoroacetate

Two fully automated synthetic procedures of [¹⁸F]fluoroacetate ([¹⁸F]FAC) have been developed using a modified commercial TRACERlab FX_FN synthesizer. One was a two‐step one‐pot procedure, consisting of nucleophilic [¹⁸F]fluorination of benzyl‐2‐bromoacetate as a precursor with no‐carrier‐added [¹⁸F]fluoride, hydrolysis within the same [¹⁸F]fluorination reaction vessel, and purification with/without high‐performance liquid chromatography (HPLC). The second procedure consisted of nucleophilic [¹⁸F]fluorination, hydrolysis on the column, and purification with SEP‐PAK cartridges instead of HPLC. The radiochemical purity of [¹⁸F]FAC was >95% by the two procedures. The second procedure was a simple, rapid, and fully automated synthesis of [¹⁸F]FAC with a high and reproducible radiochemical yield exceeding 60% (decay uncorrected) within the total synthesis time less than 20 min. The new, simple, and rapid on‐column hydrolysis procedure should be adaptable to the fully automated synthesis of [¹⁸F]FAC at a commercial fluoro‐deoxyglucose synthesis module. Copyright © 2008 John Wiley & Sons, Ltd.     

Vacuum ultraviolet photon–mediated production of [18F]F2

The chemistry of F₂ and its derivatives are amenable to facile aliphatic or aromatic substitution, as well as electrophilic addition. The main limitation in the use of [¹⁸F]F₂ for radiopharmaceutical synthesis is the low specific activity achieved by the traditional methods of production. The highest specific activities, 55 GBq/μmol, for [¹⁸F]F₂ have been achieved so far by using electrical discharge in the post‐target production of [¹⁸F]F₂ gas from [¹⁸F]CH₃F. We demonstrate that [¹⁸F]F₂ is produced by illuminating a gas mixture of neon/F₂/[¹⁸F]CH₃F with vacuum ultraviolet photons generated by an excimer laser. We tested several illumination chambers and production conditions. The effects of the initial amount of [¹⁸F]F^‐, amount of carrier F₂, and number of 193‐nm laser pulses at constant power were evaluated regarding radiochemical yield and specific activity. The specific activity attained for [¹⁸F]F₂‐derived [¹⁸F]NFSi was 10.3 ± 0.9 GBq/μmol, and the average radiochemical yield over a wide range of conditions was 6.7% from [¹⁸F]F^‐. The production can be improved by optimization of the synthesis device and procedures. The use of a commercially available excimer laser and the simplicity of the process can make this method relatively easy for adaptation in radiochemistry laboratories.     

Baeyer‐Villiger oxidation tuned to chemoselective conversion of non‐activated [18F]fluorobenzaldehydes to [18F]fluorophenols

A reaction pathway via oxidation of [¹⁸F]fluorobenzaldehydes offers a very useful tool for the no‐carrier‐added radiosynthesis of [¹⁸F]fluorophenols, a structural motive of several potential radiopharmaceuticals. A considerably improved chemoselectivity of the Baeyer‐Villiger oxidation (BVO) towards phenols was achieved, employing 2,2,2‐trifluoroethanol as reaction solvent in combination with Oxone or m‐CPBA as oxidation agent. The studies showed the necessity of H₂SO₄ addition, which appears to have a dual effect, acting as catalyst and desiccant. For example, 2‐[¹⁸F]fluorophenol was obtained with a RCY of 97% under optimised conditions of 80°C and 30‐minute reaction time. The changed performance of the BVO, which is in agreement with known reaction mechanisms via Criegee intermediates, provided the best results with regard to radiochemical yield (RCY) and chemoselectivity, i.e. formation of [¹⁸F]fluorophenols rather than [¹⁸F]fluorobenzoic acids. Thus, after a long history of the BVO, the new modification now allows an almost specific formation of phenols, even from electron‐deficient benzaldehydes. Further, the applicability of the tuned, chemoselective BVO to the n.c.a. level and to more complex compounds was demonstrated for the products n.c.a. 4‐[¹⁸F]fluorophenol (RCY 95%; relating to 4‐[¹⁸F]fluorobenzaldehyde) and 4‐[¹⁸F]fluoro‐m‐tyramine (RCY 32%; relating to [¹⁸F]fluoride), respectively.     

Synthesis of [18F]‐6‐deoxy‐6‐fluoro‐D‐glucose ([18F]6FDG), a potential tracer of glucose transport

With the goal of developing a PET radioligand for the in vivo assessment of glucose transport, 6-deoxy-6-[¹⁸F]fluoro-D -glucose ([¹⁸F]6FDG) was prepared in two steps from ¹⁸F⁻. Starting with D -glucose, the tosyl- and mesyl-derivatives of 3,5-O-benzylidene-1,2-O-isopropylidene-α-D -glucofuranose were prepared by known methods. Reaction of either of these precursors with ¹⁸F⁻ resulted in the formation of 3,5-O-benzylidene-6-deoxy-6-[¹⁸F]-fluoro-1,2-O-isopropylidene-α-D -glucofuranose in high yield. Subsequent hydrolysis resulted in the production of [¹⁸F]6FDG. Under optimal conditions, [¹⁸F]6FDG is produced 60–70 min after end of bombardment (EOB) in 71 ± 12% yield (decay corrected, based upon fluoride) with a radiochemical purity of ⩾96%. Preliminary experiments have indicated that [¹⁸F]6FDG may be a more representative in vivo tracer for the glucose transporter than 2FDG. Copyright © 2005 John Wiley & Sons, Ltd.     

Automated synthesis and purification of [18F]fluoro‐[di‐deutero]methyl tosylate

Automated synthetic procedures of [¹⁸F]fluoro‐[di‐deutero]methyl tosylate on a GE TRACERlab FX F‐N module and a non‐commercial synthesis module have been developed. The syntheses included azeotropic drying of the [¹⁸F]fluoride, nucleophilic ¹⁸F‐fluorination of bis(tosyloxy)‐[di‐deutero]methane, HPLC purification and subsequent formulation of the synthesized [¹⁸F]fluoro‐[di‐deutero]methyl tosylate (d₂‐[¹⁸F]FMT) in organic solvents. Automation shortened the total synthesis time to 50 min, resulting in an average radiochemical yield of about 50% and high radiochemical purity (>98%). The possible application of this procedure to commercially available synthesis modules might be of significance for the production of deuterated ¹⁸F‐fluoromethylated imaging probes in the future. Copyright © 2013 John Wiley & Sons, Ltd.     

Improved synthesis of [18F]fluoromethyl tosylate,a convenient reagent for radiofluoromethylations

The utility of [¹⁸F]fluoromethyl tosylate as an [¹⁸F]fluoromethylation reagent has been reexamined. The preparation of this potentially useful compound from the reaction of bis(tosyloxy) methane with ¹⁸F‐ was reported several years ago, but it had not found use as a labeling reagent. When the reported reaction of bis(tosyloxy) methane with ¹⁸F‐ was carried out, [¹⁸F]fluoromethyl tosylate was formed along with [¹⁸F]tosyl fluoride. The product ratio depended upon reaction conditions, with the yield of [¹⁸F]fluoromethyl tosylate usually in the range of 25–40%. Addition of a small amount of water to the reaction mixture resulted in a significant increase in the yield of [¹⁸F]fluoromethyl tosylate. Reaction conditions were defined that produced a yield of 71±6% of [¹⁸F]fluoromethyl tosylate (decay corrected). The product was conveniently purified by alumina chromatography. Reaction of [¹⁸F]fluoromethyl tosylate with the (des‐fluoromethyl) fluticasone propionate thioacid precursor produced [¹⁸F]fluticasone propionate in improved yield (16%, from fluoride in production‐scale runs) over other synthesis methods. Similarly, formation of [¹⁸F]choline, [¹⁸F]fluoromethionine and N‐([¹⁸F]fluoromethyl)spiperone from the reaction of [¹⁸F]fluoromethyl tosylate with corresponding precursors was examined. Copyright © 2005 John Wiley & Sons, Ltd.     

[18F]Fluoropropylsulfonyl chloride: a new reagent for radiolabeling primary and secondary amines for PET imaging

In vivo molecular imaging with positron emission tomography (PET) requires the preparation of an appropriate positron‐emitting radiotracer. New methods for the introduction of F‐18 into biologically interesting molecules could increase the availability of specific PET radiotracers and increase the application of PET to the study of human diseases. In this work, [¹⁸F]fluoropropylsulfonyl chloride was synthesized from 3‐toluenesulfonyloxypropyl thiocyanate in two steps and was successfully incorporated into molecules containing a reactive amino group. Both a primary amine, L‐phenylalanine ethyl ester hydrochloride, and a secondary amine, 1‐(2‐methoxyphenyl)‐piperazine, were successfully radiolabeled by this method. The entire radiochemical synthesis required 90 min. The products were obtained in 25.7±2.3% (n=3) and 22.8±9.1% (n=6) (EOB). This method provides a useful and easy way to make new F‐18 labeled radiopharmaceuticals for PET imaging. Copyright © 2008 John Wiley & Sons, Ltd.     

Syntheses of meta-[F]Fluorobenzaldehyde and meta-[F]Fluorobenzylbromide from Phenyl(3-Formylphenyl) Iodonium Salt Precursors

¹⁸F‐labeled fluorobenzaldehydes and fluorobenzylbromides are useful synthons for the preparation of positron emission tomography radiopharmaceuticals. Although ortho‐ and para‐[¹⁸F]fluorobenzaldehydes can easily be prepared with high yields, the corresponding meta‐derivatives are more problematic. In order to improve the yield of meta‐[¹⁸F]fluorobenzaldehyde, we used the corresponding diaryliodonium salt precursors, since diaryliodonium salts had already been used as precursors in the preparations of ¹⁸F‐labeled electron‐rich, as well as electron‐deficient, aromatic rings. Diaryliodonium salts with different counter ions [PhIPhCHO]X (X = Cl, Br, OTs, OTf) were synthesized. ¹⁸F radiolabeling was performed using different bases at different temperatures in the presence of a radical scavenger, 2,2,6,6‐tetramethylpiperidine‐N‐oxyl (TEMPO). The best conversion (～80%) to meta‐[¹⁸F]fluorobenzaldehyde was obtained using CsHCO₃ base at a reaction temperature of 110°C. To study iodonium salt counter ion effects on radiofluorination, each precursor was separately treated with Cs[¹⁸F]F/CsHCO₃ in DMF at 110°C for 5 min in the presence of TEMPO. Our observed reactivity order was OTsMeta‐[¹⁸F]fluorobenzaldehyde thus obtained was reduced to the corresponding alcohol with aqueous NaBH₄ at room temperature and then converted to meta‐[¹⁸F]fluorobenzylbromide using triphenylphosphine dibromide. Formation of meta‐[¹⁸F]fluorobenzylbromide was confirmed using high‐performance liquid chromatography and the desired product was purified on a silica Sep ‐ Pak^® plus cartridge. Published in 2011 by John Wiley & Sons, Ltd.     

Automated production at the curie level of no‐carrier‐added 6‐[18F]fluoro‐ l‐dopa and 2‐[18F]fluoro‐ l‐tyrosine on a FASTlab synthesizer

An efficient, fully automated, enantioselective multi‐step synthesis of no‐carrier‐added (nca) 6‐[¹⁸F]fluoro‐L‐dopa ([¹⁸F]FDOPA) and 2‐[¹⁸F]fluoro‐L‐tyrosine ([¹⁸F]FTYR) on a GE FASTlab synthesizer in conjunction with an additional high‐ performance liquid chromatography (HPLC) purification has been developed. A PTC (phase‐transfer catalyst) strategy was used to synthesize these two important radiopharmaceuticals. According to recent chemistry improvements, automation of the whole process was implemented in a commercially available GE FASTlab module, with slight hardware modification using single use cassettes and stand‐alone HPLC. [¹⁸F]FDOPA and [¹⁸F]FTYR were produced in 36.3 ± 3.0 % (n = 8) and 50.5 ± 2.7 % (n = 10) FASTlab radiochemical yield (decay corrected). The automated radiosynthesis on the FASTlab module requires about 52 min. Total synthesis time including HPLC purification and formulation was about 62 min. Enantiomeric excesses for these two aromatic amino acids were always >95 %, and the specific activity of was >740 GBq/µmol. This automated synthesis provides high amount of [¹⁸F]FDOPA and [¹⁸F]FTYR (>37 GBq end of synthesis (EOS)). The process, fully adaptable for reliable production across multiple PET sites, could be readily implemented into a clinical good manufacturing process (GMP) environment.     

Synthesis of a phenolic precursor and its efficient O‐[18F]fluoroethylation with purified no‐carrier‐added [18F]2‐fluoroethyl brosylate as the labeling agent

[¹⁸F]2‐Fluoroethyl‐p‐toluenesulfonate also called [¹⁸F]2‐fluoroethyl tosylate has been widely used for labeling radioligands for positron emission tomography (PET). [¹⁸F]2‐Fluoroethyl‐4‐bromobenzenesulfonate, also called [¹⁸F]2‐fluoroethyl brosylate ([¹⁸F]F(CH₂)₂OBs), was used as an alternative radiolabeling agent to prepare [¹⁸F]FEOHOMADAM, a fluoroethoxy derivative of HOMADAM, by O‐fluoroethylating the phenolic precursor. Purified by reverse‐phase HPLC, the no‐carrier‐added [¹⁸F]F(CH₂)₂OBs was obtained in an average radiochemical yield (RCY) of 35%. The reaction of the purified and dried [¹⁸F]F(CH₂)₂OBs with the phenolic precursor was performed by heating in DMF and successfully produced [¹⁸F]FEOHOMADAM, after HPLC purification, in RCY of 21%. Copyright © 2013 John Wiley & Sons, Ltd.     

[18F]Fluoride labelling of macromolecules in aqueous conditions: silicon and boroaryl‐based [18F]fluorine acceptors, [18F]FDG conjugation and Al18F chelation

[¹⁸F]Fluorination is usually carried out by nucleophilic substitution reactions entailing the use of stringent conditions. A number of novel techniques including silicon and boron‐based fluoride acceptor molecules, [¹⁸F]fluoro‐2‐deoxy‐ d ‐glucose and chelation of the Al¹⁸F complex have been employed recently to achieve [¹⁸F]radiolabelling of macromolecules. These approaches are reviewed herein. Copyright © 2012 John Wiley & Sons, Ltd.     

Synthesis of [18F]fluoroacetaldehyde. Application to [18F]fluoroethylation of benzylamine under reductive alkylation conditions

The radiosynthesis of a new [¹⁸F]fluoroalkylating agent, [¹⁸F]fluoroacetaldehyde, is described. It was produced using the Kornblum method by oxidation with dimethyl sulphoxide of 2‐[¹⁸F]fluoroethyl p‐toluenesulphonate ([¹⁸F]FETos). In these conditions the oxidation proceeds smoothly and rapidly to the selective conversion of tosyl esters of primary alcohols to aldehydes with no carboxylic acids being produced. The chemical identity of [¹⁸F]fluoroacetaldehyde was determined by comparing its chromatographic properties as well as those of its 2,4‐dinitrophenylhydrazone (2,4‐DNPH) derivative with those of, respectively, the standard fluoroacetaldehyde and its 2,4‐DNPH derivative. Standard fluoroacetaldehyde was prepared by oxidation of fluoroethanol with pyridinium dichromate and characterized as its 2,4‐DNPH derivative by mass spectrometry. To test its reactivity with amines under reductive alkylation conditions, [¹⁸F]fluoroacetaldehyde was reacted with benzylamine used as model substrate. The chemical identity of the resulting radiolabelled product was determined to be [¹⁸F]N‐(2‐fluoroethyl)‐benzylamine by comparing its chromatographic properties with those of the synthesized standard N‐(2‐fluoroethyl)‐benzylamine characterized by ¹⁹F and ¹H NMR spectroscopy and mass spectrometry. This new fluorine‐18 labelled synthon may find applications in radiolabelling peptide, protein and antibody fragments as well as in aldol condensation or in the Mannich reaction. Copyright © 2008 John Wiley & Sons, Ltd.     

Automated synthesis of N‐(2‐[18F]Fluoropropionyl)‐l‐glutamic acid as an amino acid tracer for tumor imaging on a modified [18F]FDG synthesis module

N‐(2‐[¹⁸F]Fluoropropionyl)‐l ‐glutamic acid ([¹⁸F]FPGLU) is a potential amino acid tracer for tumor imaging with positron emission tomography. However, due to the complicated multistep synthesis, the routine production of [¹⁸F]FPGLU presents many challenging laboratory requirements. To simplify the synthesis process of this interesting radiopharmaceutical, an efficient automated synthesis of [¹⁸F]FPGLU was performed on a modified commercial fluorodeoxyglucose synthesizer via a 2‐step on‐column hydrolysis procedure, including ¹⁸F‐fluorination and on‐column hydrolysis reaction. [¹⁸F]FPGLU was synthesized in 12 ± 2% (n = 10, uncorrected) radiochemical yield based on [¹⁸F]fluoride using the tosylated precursor 2 . The radiochemical purity was ≥98%, and the overall synthesis time was 35 minutes. To further optimize the radiosynthesis conditions of [¹⁸F]FPGLU, a brominated precursor 3 was also used for the preparation of [¹⁸F]FPGLU, and the improved radiochemical yield was up to 20 ± 3% (n  = 10, uncorrected) in 35 minutes. Moreover, all these results were achieved using the similar on‐column hydrolysis procedure on the modified fluorodeoxyglucose synthesis module.     

Degradation of acetonitrile in eluent solutions for [18F]fluoride PET chemistry: impact on radiosynthesis of [18F]FACBC and [18F]FDG

In [¹⁸F]fluoride chemistry, an eluent solution containing a weak aqueous base is used to release [¹⁸F]fluoride after adsorption on an anion exchange resin. Traditionally, the eluent solution is freshly prepared, but modern PET tracer manufacturers may utilize the benefits of preparing bulk solutions or prefilled vials for storage. We discovered that typical eluent solutions containing kryptofix and K₂CO₃ in aqueous acetonitrile degraded upon storage. Acetonitrile will at alkaline pH hydrolyse to acetamide and ammonium acetate. Acetate may serve as a competing nucleophile to [¹⁸F]fluoride. Eluent solutions used in the synthesis of [¹⁸F]FACBC and [¹⁸F]FDG generated mg/ml levels of acetamide and ammonium acetate during storage at room temperature or above. The synthesis of [¹⁸F]FACBC was prone to eluent degradation, with gradual reduction of radiochemical yield (RCY) from 62.5% to 44.7% during 12 months of storage at 30 °C. The synthesis of [¹⁸F]FDG was only affected when the eluent was stored at 50 °C, reducing the RCY from 86.8% to 66.7% after 3 months of storage. For degradation effects to be avoided, an alternative eluent solution with no acetonitrile was investigated in the synthesis of [¹⁸F]FACBC. A methanol‐based eluent was successfully made, showing no degradation and unchanged RCY after 6 months of storage at 50 °C. Copyright © 2012 John Wiley & Sons, Ltd.     

Fine‐tuning of the automated [18F]PSMA‐1007 radiosynthesis

Radiolabeled prostate‐specific membrane antigen (PSMA) targeting PET‐tracers have become desirable radiopharmaceuticals for the imaging of prostate cancer (PC). Recently, the PET radiotracer [¹⁸F]PSMA‐1007 was introduced as an alternative to [⁶⁸Ga]Ga‐PSMA‐11, for staging and diagnosing biochemically recurrent PC. We incorporated a one‐step procedure for [¹⁸F]PSMA‐1007 radiosynthesis, using both Synthra RNplus and GE TRACERlab FxFN automated modules, in accordance with the recently described radiolabeling procedure. Although the adapted [¹⁸F]PSMA‐1007 synthesis resulted in repeatable radiochemical yields (55 ± 5%, NDC), suboptimal radiochemical purities of 87 ± 8% were obtained using both modules. As described here, modifications made to the radiolabeling and the solid‐phase extraction purification steps reduced synthesis time to 32 minutes and improved radiochemical purity to 96.10%, using both modules, without shearing the radiochemical yield.     

自动化合成N-琥珀酰亚胺-4-[18F]氟苯甲酸酯

目的 合成18F同位素标记蛋白质、配体、多肽类的中间体N-琥珀酰亚胺-4-[18F]氟苯甲酸酯(18F-FB).方法 以乙基-4-三甲胺苯甲酸酯-三氟磺酸盐为反应前体,利用正电子发射断层成像(PET)显像药物2-氟-18-氟-2-脱氧-D-葡萄糖(18F-FDG)合成专用模块TRACERlab FX-FDG和多用合成模块TRACERlab FX-FN及其固相萃取系统,基于控制软件的改造,通过亲核取代、氢氧化钠水解、酯化反应"三步法"合成.结果 合成18F-FB的总放射性合成时间小于80 min,校正后放射化学产率(38±3)%(n=10),放射化学纯度＞99%,与标准品19F-FB行HPLC比对分析,在柱平均保留时间Tr=8.515 min,两者保留时间基本吻合.结论 此法可以成功合成18F-FB,合成工艺成熟稳定,完全实现了自动化合成,为成功实现18F同位素标记蛋白、多肽类大分子物质进而实现PET成像提供了良好条件.     

A one-pot radiosynthesis of [18F]PARPi

In this paper, we disclose a new strategy for the radiosynthesis of [¹⁸F]PARPi from the corresponding, boc-protected, nitro-precursor. Using a two-step procedure, [¹⁸F]PARPi could be isolated in radiochemical yields up to 9.6%. The reaction proceeds via an efficient one-pot, two-step process, allowing for simplification over previous methods that require complex multi-step, multi-pot strategies to be implemented.