C07B59/001

Method of fabricating [F-18]FEONM

A PET imaging agent is made, by at first, washing out fluoride ions (F-18) adhered on an ion exchange resin to a reaction vessel with potassium carbonate/Kryptofix 2.2.2 in acetonitrile-water. After processing the first azeotropic distillation with helium while water is removed, the temperature is cooled down. Then, acetonitrile is added to the reaction vessel to be heated up. After processing the second azeotropic distillation with helium while water is removed, the temperature is cooled down and excess water is extracted. A precursor is then added to the reaction vessel to be heated up for processing a fluorination reaction. The reaction mixture obtained after the fluorination reaction is cooled down to be flown through a solid-phase extraction column with waste drained into a waste tank. Then, ethanol is used to wash out a product, i.e. [F-18]FEONM, adsorbed by the column, to be collected in a collection vial.

Labeled chiral alpha-hydroxy ketoacid derivatives, a process for preparing said derivatives and their use

The present invention relates to labeled chiral alpha-hydroxy ketoacid derivatives, a process for preparing the derivatives and their use for isotopic labeling of amino acids, in particular, for isotopic labeling of methyl groups of amino acids, and more particularly, for specific isotopic labeling of valine, leucine and isoleucine methyl groups, in proteins and biomolecular assemblies. The invention also concerns a process for analyzing proteins and biomolecular assemblies by NMR spectroscopy including a step of isotopic labeling of amino acids, in particular, valine, leucine and isoleucine, in proteins and biomolecular assemblies to be analyzed by the chiral alpha-hydroxy ketoacid derivatives of the invention. The invention further relates to a kit for isotopic labeling of valine, leucine and isoleucine amino acids, in proteins and biomolecular assemblies including one or more chiral alpha-hydroxy ketoacid derivatives of the invention.

Method for preparing methylated amines

The present invention relates to a method for preparing methylated amines using carbon dioxide and to the use of the method for manufacturing vitamins, pharmaceutical products, glues, acrylic fibres and synthetic leathers, pesticides and fertilisers. The invention also relates to a method for manufacturing vitamins, pharmaceutical products, glues, acrylic fibres, synthetic leathers, pesticides and fertilisers, including a step of preparing methylated amines by the method according to the invention. The present invention also relates to a method for preparing marked methylated amines and to the uses thereof.

18F-TAGGED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer.

Synthesizing pet tracers using [F-18]sulfonyl fluoride as a source of [F-18]fluoride
11242314 · 2022-02-08 · ·

The present disclosure relates to the methods for the preparation of reactive [F-18]fluoride in a form of [F-18]sulfonyl fluoride suitable for efficient radiolabeling without an azeotropic evaporation step by the use of anion exchange resin and sulfonyl chloride, and its applications in the manufacturing of PET radiopharmaceuticals.

METAL OXIDE CATALYZED RADIOFLUORINATION

Inter alia, the first titania-catalyzed [.sup.18F]-radiofluorination in highly aqueous medium is provided. In embodiments, the method utilizes titanium dioxide, 1:1 acetonitrile-thexyl alcohol solvent mixture and tetrabutylammonium bicarbonate as a base. Radiolabeling may be directly performed with aqueous [.sup.18F]fluoride without the need for drying/azeotroping step, which reduces radiosynthesis time while keeping high fluoride conversion. The general applicability of the synthetic strategy to the synthesis of the wide range of PET probes from tosylated precursors is demonstrated.

Organic electroluminescent element, material for organic electroluminescent element and light emitting device, display device, and illumination device, each employing organic electroluminescent element

This application relates in part to an organic electroluminescent element including a substrate, a pair of electrodes including an anode and a cathode, disposed on the substrate, and an organic layer(s) including a light emitting layer, in which the organic layer(s) contains a compound represented by the following formula (1), in which R.sup.1 to R.sup.8 are each hydrogen or a substituent, at least one of R.sup.1 to R.sup.4 and at least one of R.sup.5 to R.sup.8 are each a substituent represented by the formula (2); R.sup.9 to R.sup.12, Z.sup.1 to Z.sup.4, Ar.sup.1, Ar.sup.2, and L.sup.1 are as defined herein. ##STR00001##

Multi-Enzyme Nanoparticle-Assisted Stable Isotope Incorporation Into Small Molecules by Channeling

Multi-enzyme systems attached to nanoparticles are effective to efficiently and controllably incorporate stable isotopes (such as deuterium) during the synthesis of small molecules. In one example, deuterium is incorporated into (+)-dihydrocarvide using a cascade involving the enzymes (a) pentaerythritol tetranitrate reductase (PETNR) and (b) flavin-dependent cyclohexanone monooxygenase triple variant F249A/F280A/F435A (CHMO.sub.3M).

Ligands for imaging cardiac innervation

Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release thereby reducing side effects, improved quantitative data, and/or high affinity for VMAT over prior radiotracers. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

PROCESS FOR THE SPECIFIC ISOTOPIC LABELING OF METHYL GROUPS OF VAL, LEU AND ILE

A process for the specific isotopic labeling of an amino acid selected from Valine (Val), Leucine (Leu), and Isoleucine (Ile), in proteins and biomolecular assemblies by introducing, in a medium containing bacteria overexpressing a protein, an acetolactate derivative of Formula I of the application.