Category: 757982-31-3

Wright, Jay S. published the artcileSequential Ir/Cu-Mediated Method for the Meta-Selective C-H Radiofluorination of (Hetero)Arenes, Name: Methyl 4-fluoro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate, the publication is Journal of the American Chemical Society (2021), 143(18), 6915-6921, database is CAplus and MEDLINE.

This article describes a sequential Ir/Cu-mediated process for the meta-selective C-H radiofluorination of (hetero)arene substrates. In the first step, Ir-catalyzed C(sp²)-H borylation affords (hetero)aryl pinacolboronate (BPin) esters. The intermediate organoboronates are then directly subjected to copper-mediated radiofluorination with [¹⁸F]tetrabutylammonium fluoride to afford fluorine-18 labeled (hetero)arenes in high radiochem. yield and radiochem. purity. This entire process is performed on a bench top without Schlenk or glove box techniques and circumvents the need to isolate (hetero)aryl boronate esters. The reaction was automated on a TracerLab FX_FN module with 1,3-dimethoxybenzene and a meta-tyrosine derivative The products, [¹⁸F]1-fluoro-3,5-dimethoxybenzene and an ¹⁸F-labeled meta-tyrosine derivative, were obtained in 37 ± 5% isolated radiochem. yield and >99% radiochem. purity and 25% isolated radiochem. yield and 99% radiochem. purity, and 0.52 Ci/μmol (19.24 GBq/μmol) molar activity (A_m), resp.

Journal of the American Chemical Society published new progress about 757982-31-3. 757982-31-3 belongs to esters-buliding-blocks, auxiliary class Boronic acid and ester,Boronic acid and ester, name is Methyl 4-fluoro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate, and the molecular formula is C21H26Br4S2, Name: Methyl 4-fluoro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Takaya, Jun published the artcileFluorine-controlled C-H borylation of arenes catalyzed by a PSiN-pincer platinum complex, COA of Formula: C14H18BFO4, the publication is Chemical Communications (Cambridge, United Kingdom) (2015), 51(100), 17662-17665, database is CAplus and MEDLINE.

An efficient, regioselective synthesis of fluorine-substituted arylboronic esters was achieved through fluorine-controlled C-H borylation of arenes with diboron catalyzed by a PSiN-platinum complex. The promising utility of the PSiN-platinum catalyst and its unique regioselectivity were demonstrated for the first time, which would complement the well-developed Ir-catalyzed C-H borylation.

Chemical Communications (Cambridge, United Kingdom) published new progress about 757982-31-3. 757982-31-3 belongs to esters-buliding-blocks, auxiliary class Boronic acid and ester,Boronic acid and ester, name is Methyl 4-fluoro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate, and the molecular formula is C34H33ClN6O7, COA of Formula: C14H18BFO4.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Gracia, Jordi published the artcileBiphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships, Name: Methyl 4-fluoro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate, the publication is Journal of Medicinal Chemistry (2016), 59(23), 10479-10497, database is CAplus and MEDLINE.

Cyclic nucleotide cAMP is an ubiquitous second messenger involved in a plethora of cellular responses to biol. agents involving activation of adenylyl cyclase. Its intracellular levels are tightly controlled by a family of cyclic nucleotide degrading enzymes, the PDEs. In recent years, cyclic nucleotide phosphodiesterase type 4 (PDE4) has aroused scientific attention as a suitable target for anti-inflammatory therapy in respiratory diseases, particularly in the management of asthma and COPD. Here the authors describe efforts to discover novel, highly potent inhaled inhibitors of PDE4. Through structure based design, with the intervention of a wide variety of functional groups and physichochem. profiles to occupy the solvent-filled pocket of the PDE4 enzyme, the authors modified the structure of the authors’ oral PDE4 inhibitors to reach compounds up to picomolar enzymic potencies. In vitro potencies were demonstrated in a rat lung neutrophilia model by suspension microspray administration.

Journal of Medicinal Chemistry published new progress about 757982-31-3. 757982-31-3 belongs to esters-buliding-blocks, auxiliary class Boronic acid and ester,Boronic acid and ester, name is Methyl 4-fluoro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate, and the molecular formula is C14H18BFO4, Name: Methyl 4-fluoro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics