F-Fluorination of a supported 2-(aryl-di-tert-butylsilyl)-N-methyl-imidazole for indirect F-labeling of a V H single-variable domain.

Anchoring an imidazole-di-tert-butyl-arylsilane possessing an azido group to a polystyrene resin provided a heterogeneous precursor that was radiolabeled easily using aqueous [ F]fluoride. After optimizing the conditions (i.e.

Last-step F-fluorination of supported 2-(aryl-di--butylsilyl)--methyl-imidazole conjugates for applications in positron emission tomography.

Aiming for potential applications in positron emission tomography, fully automated productions of F-labelled bioconjugates were achieved using heterogenous precursors obtained by anchoring imidazole-di--butyl-arylsilanes to a polystyrene resin. The reactions were performed using either "batch" or "flow" procedures, avoiding both the time-consuming azeotropic drying and HPLC purifications usually required.

Translational strategy using multiple nuclear imaging biomarkers to evaluate target engagement and early therapeutic efficacy of SAR439859, a novel selective estrogen receptor degrader.

Purpose: Preclinical in vivo nuclear imaging of mice offers an enabling perspective to evaluate drug efficacy at optimal dose and schedule. In this study, we interrogated sufficient estrogen receptor occupancy and degradation for the selective estrogen receptor degrader (SERD) compound SAR439859 using molecular imaging and histological techniques.

Material And Methods: [F]FluoroEstradiol positron emission tomography (FES-PET), [F]FluoroDeoxyGlucose (FDG) PET, and [F]FluoroThymidine (FLT) PET were investigated as early pharmacodynamic, tumor metabolism, and tumor proliferation imaging biomarkers, respectively, in mice bearing subcutaneous MCF7-Y537S mutant ERα+ breast cancer model treated with the SERD agent SAR439859.

The first radiosynthesis of 2-amino-5-[F]fluoropyridines via a "minimalist" radiofluorination/palladium-catalyzed amination sequence from anisyl(2-bromopyridinyl)iodonium triflate.

The synthesis of 2-amino-5-[F]fluoropyridines was achieved in 8-85% yields by palladium-catalyzed reaction of 2-bromo-5-[F]fluoropyridine with piperidine, dimethylamine, butylamine, methylpiperazine, benzylamine, aniline and 3-aminopyridine. 2-Bromo-5-[F]fluoropyridine was obtained by radiofluorination of anisyl(2-bromopyridinyl-5)iodonium triflate (88% yield). The radiofluorination step was performed under "minimalist" conditions to guarantee a successful subsequent amination reaction.

Alpha,beta-unsaturated delta-lactones from copper-catalyzed asymmetric vinylogous Mukaiyama reactions of aldehydes: scope and mechanistic insights.

A direct regio-, diastereo-, and enantiocontrolled access to alpha,beta-unsaturated delta-lactones is described, based on the reaction of a silyl dienolate and an aldehyde in the presence of 10 % of Carreira's catalyst. The scope and limitations of this reaction, as well as mechanistic insights concerning the reactivity of an allyl copper species, are discussed.