Catharina Neudorfer

Green Solvents in Organic Synthesis: An Overview

Research concerning green solvents is focused on reducing environmental damages due to the use of toxic solvents in organic chemistry. Hence, there have been developed a lot of solvent-free processes as well as more efficient recycling protocols in the last dec- ades. Unfortunately, these approaches have their limitations. Therefore, the authors review different environmentally benign solvent al- ternatives. This report highlights reactions using water, fluorous solvents, ionic liquids, organic carbonates, supercritical carbon dioxide, as well as biosolvents instead of conventional organic solvents.

Syntheses of Precursors and Reference Compounds of the Melanin-Concentrating Hormone Receptor 1 (MCHR1) Tracers [11C]SNAP-7941 and [18F]FE@SNAP for Positron Emission Tomography

The MCH receptor has been revealed as a target of great interest in positron emission tomography imaging. The receptor′s eponymous substrate melanin-concentrating hormone (MCH) is a cyclic peptide hormone, which is located predominantly in the hypothalamus with a major influence on energy and weight regulation as well as water balance and memory. Therefore, it is thought to play an important role in the pathophysiology of adiposity, which is nowadays a big issue worldwide. Based on the selective and high-affinity MCH receptor 1 antagonist SNAP-7941, a series of novel SNAP derivatives has been developed to provide different precursors and reference compounds for the radiosyntheses of the novel PET radiotracers [11C]SNAP-7941 and [18F]FE@SNAP. Positron emission tomography promotes a better understanding of physiologic parameters on a molecular level, thus giving a deeper insight into MCHR1 related processes as adiposity.

Development of potential selective and reversible pyrazoline based MAO-B inhibitors as MAO-B PET tracer precursors and reference substances for the early detection of Alzheimer's disease.

Since high MAO-B levels are present in early stages of AD, the MAO-B system can be designated as an appropriate and prospective tracer target of molecular imaging biomarkers for the detection of early AD. According to the preceding investigations of Mishra et al. the aim of this work was the development of a compound library of selective and reversible MAO-B inhibitors by performing bioisosteric modifications of the core structure of 3-(anthracen-9-yl)-5-phenyl-4,5-dihydro-1H-pyrazoles. In conclusion, 13 new pyrazoline based derivatives have been prepared, which will serve as precursor substances for future radiolabeling as well as reference compounds for the investigation of increased MAO-B levels in AD.

1-(3-Amino-1-phenylpropyl)-3-(2-fluorophenyl)-1,3-dihydro-2H-benzimidazol-2-one

Starting from 1-(2-fluorophenyl)-1,3-dihydro-2H-benzimidazol-2-one (1) and (1-bromo-3-chloropropyl)benzene (2), the target compound 3, which represents a precursor for future radiolabeling, is prepared in a three-step synthesis.

A one-step microwave-assisted synthetic method for an O/S-chemoselective route to derivatives of the first adenosine A3 PET radiotracer.

The synthesis of reference standards and expected in vivo metabolites of the first adenosine A3 PET radiotracer [18F]FE@SUPPY [18F]fluoroethyl 4,6-diethyl-5-[(ethyl-sulfanyl)carbonyl]-2-phenylpyridine-3-carboxylate) was achieved by using a straightforward microwave assisted alkylation method, which allowed O/S-chemoselective alkylation of the starting material 1 to give each target compound 2–8 in a single step.