Recovery of Gallium-68 and Zinc from HNO-Based Solution by Liquid-Liquid Extraction with Arylamino Phosphonates.

The cyclotron production of gallium-68 via the Zn()Ga nuclear reaction in liquid targets is gaining significant traction in clinics. This work describes (1) the synthesis of new arylamino phosphonates via the Kabachnik-Fields reaction, (2) their use for liquid-liquid extraction of Ga from 1 M Zn(NO)/0.01 M HNO in batch and continuous flow, and (3) the use of Raman spectroscopy as a process analytical technology (PAT) tool for in-line measurement of Zn.

Novel Bifunctional [16]aneS-Derived Chelators for Soft Radiometals.

The field of targeted radionuclide therapy is rapidly growing, highlighting the need for wider radionuclide availability. Soft Lewis acid ions, such as radioisotopes of platinum, rhodium and palladium, are particularly underdeveloped. This is due in part to a lack of compatible bifunctional chelators.

Theranostic Radiopharmaceuticals Targeting Cancer-Associated Fibroblasts.

The tumor microenvironment is a dynamic ecosystem where malignant cells interact with the stromal cells sustaining and promoting tumor growth and metastasis. Cancer-associated fibroblasts (CAFs) are the major component of tumor stroma. CAFs control key tumorigenic activities by participating in immune evasion and suppression, extracellular matrix remodeling, neo-angiogenesis, and drug resistance.

IAEA contribution to the development of 64Cu radiopharmaceuticals for theranostic applications.

Copper-64 is a very attractive radioisotope with unique nuclear properties that allow using it as both a diagnostic and therapeutic agent, thus providing an almost ideal example of a theranostic radionuclide. A characteristic of Cu-64 stems from the intrinsic biological nature of copper ions that play a fundamental role in a large number of cellular processes. Cu-64 is a radionuclide that reflects the natural biochemical pathways of Cu-64 ions, therefore, can be exploited for the detection and therapy of certain malignancies and metabolic diseases.

Design, Synthesis, Computational, and Preclinical Evaluation of Ti/Ti-Labeled Urea-Based Glutamate PSMA Ligand.

Despite promising anti-cancer properties in vitro, all titanium-based pharmaceuticals have failed in vivo. Likewise, no target-specific positron emission tomography (PET) tracer based on the radionuclide Ti has been developed, notwithstanding its excellent PET imaging properties. In this contribution, we present liquid-liquid extraction (LLE) in flow-based recovery and the purification of Ti, computer-aided design, and the synthesis of a salan-Ti/Ti-chelidamic acid (CA)-prostate-specific membrane antigen (PSMA) ligand containing the Glu-urea-Lys pharmacophore.

A solid support generator of the Auger electron emitter rhodium-103m from [Pd]palladium.

Auger electron therapy is an attractive modality for targeting microscopic tumors. Rhodium-103 m (Rh, T = 56.1 min) is a promising Auger electron emitter that can be obtained as the decay product of palladium-103 (Pd, T = 16.

Bringing Radiotracing to Titanium-Based Antineoplastics: Solid Phase Radiosynthesis, PET and ex Vivo Evaluation of Antitumor Agent [(45)Ti](salan)Ti(dipic).

We present a novel solid-phase based (45)Ti radiolabeling methodology and the implementation of (45)Ti-PET in titanium-based antineoplastics using the showcase compound [(45)Ti](salan)Ti(dipic). This development is intended to allow elucidation of the biodistribution and pharmacokinetics of promising new Ti-based therapeutics.

Automated synthesis and PET evaluation of both enantiomers of [¹⁸F]FMISO.

Introduction: [(18)F]FMISO, the widely used positron emission tomography (PET) hypoxia tracer, is a chiral compound clinically used as a racemic mixture. The purpose of this study was to synthesize the individual (R)- and the (S)- enantiomers of [(18)F]FMISO and compare their PET imaging characteristics.

Methods: The radiosynthesis of enantiopure (R)- and (S)-[(18)F]FMISO was based on Co(salen) (N,N'-bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexanediaminocobalt)-mediated opening of enantiopure epoxides with [(18)F]HF.

Automated solid-phase radiofluorination using polymer-supported phosphazenes.

The polymer supported phosphazene bases PS-P₂(tBu) and the novel PS-P₂(PEG) allowed for efficient extraction of [¹⁸F]F⁻ from proton irradiated [¹⁸O]H₂O and subsequent radiofluorination of a broad range of substrates directly on the resin. The highest radiochemical yields were obtained with aliphatic sulfonates (69%) and bromides (42%); the total radiosynthesis time was 35-45 min. The multivariate analysis showed that the radiochemical yields and purities were controlled by the resin load, reaction temperature, and column packing effects.

Homogeneous nucleophilic radiofluorination and fluorination with phosphazene hydrofluorides.

A series of phosphazenium hydrofluorides, P(1)(tBu)·[(18/19)F]HF, P(1)(tOct)·[(18/19)F]HF, P(2)(Et)·[(18/19)F]HF, and P(4)(tBu)·[(18/19)F]HF, was synthesized. The radioactive phosphazenium [(18)F]hydrofluorides were obtained by the one-step formation and trapping of gaseous [(18)F]HF with the respective phosphazene bases. The [(19)F] isotopomers were prepared from the corresponding phosphazene bases and Et(3)N·3HF.

Electronic structure and chain-length effects in diplatinum polyynediyl complexes trans,trans-[(X)(R3P)2Pt(C triple bond C)(n)Pt(PR3)2(X)]: a computational investigation.

Structure and bonding in the title complexes are studied using model compounds trans,trans-[(C6H5)(H3P)2Pt(C triple bond C)(n)Pt(PH3)2(C6H5)] (PtCxPt; x = 2n = 4-26) at the B3LYP/LACVP* level of density functional theory. Conformations in which the platinum square planes are parallel are very slightly more stable than those in which they are perpendicular (DeltaE = 0.12 kcal mol(-1) for PtC8Pt).

Kinetic isotope effects in cycloreversion of rhenium (V) diolates.

Cycloreversion of 4-methoxystyrene from the corresponding Tp'Re(O)(diolato) complex (Tp' = hydrido-tris-(3,5-dimethylpyrazolyl)borate) was measured competitively for various isotopomers at 103 degrees C. Primary ((12)C/(13)C) and secondary ((1)H/(2)H) kinetic isotope effects were determined. The primary KIEs were k(12C)/k(13C) = 1.