1049730-39-3

Basic information

• Product Name: 1-(2-FLUOROETHYL)-4-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)-1 H-PYRAZOLE
• Synonyms: 1-(2-FLUOROETHYL)-4-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)-1 H-PYRAZOLE;1-(2-fluoroethyl)-4-(tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole;(1-(2-FLUOROETHYL)-1H-PYRAZOL-4-YL)BORONIC ACID PINACOL ESTER
• CAS NO: 1049730-39-3
• Molecular Formula: C11H18BFN2O2
• Molecular Weight: 240.0822232
• Mol File: 1049730-39-3.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• Storage Temp.: 2-8°C
• CAS DataBase Reference: 1-(2-FLUOROETHYL)-4-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)-1 H-PYRAZOLE(CAS DataBase Reference)
• NIST Chemistry Reference: 1-(2-FLUOROETHYL)-4-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)-1 H-PYRAZOLE(1049730-39-3)
• EPA Substance Registry System: 1-(2-FLUOROETHYL)-4-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)-1 H-PYRAZOLE(1049730-39-3)

Safety Data

• Hazardous Substances Data: 1049730-39-3(Hazardous Substances Data)

Usage

General Description

The chemical 1-(2-fluoroethyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a compound with a pyrazole ring structure and a boron-containing substituent. It is used in the field of organic chemistry as a valuable building block in the synthesis of various pharmaceuticals and agrochemicals. Its unique structure and reactivity make it suitable for use in Suzuki-Miyaura cross-coupling reactions and other organic transformations. Additionally, the fluorine substituent on the ethyl group and the tetramethyl-1,3,2-dioxaborolane group contribute to its stability and reactivity, making it a versatile and valuable compound in the field of chemical synthesis.

Upstream product

• 269410-08-4 pyrazole-4-boronic acid pinacol ester 
• 762-49-2 2-fluoroethyl bromide 
• 762-51-6 1-fluoro-2-iodoethane 

Relevant articles and documents

Evaluation of carbon-11 labeled 5-(1-methyl-1H-pyrazol-4-yl)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)nicotinamide as PET tracer for imaging of CSF-1R expression in the brain

Pharmacological targeting of tumor associated macrophages and microglia in the tumor microenvironment is a novel therapeutic strategy in the treatment of glioblastoma multiforme. As such, the colony stimulating factor-1 receptor (CSF-1R) has been identified as a druggable target. However, no validated companion diagnostic marker for these therapies exists to date. Towards development of a CSF-1R PET tracer, a set of six compounds based on recently reported CSF-1R inhibitor 5-(1-methyl-1H-pyrazol-4-yl)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)nicotinamide (Compound 5) was designed, synthesized and evaluated in vitro for potency and selectivity. The highest affinity for CSF-1R was found for compound 5 (IC50: 2.7 nM). Subsequent radiosynthesis of [11C]5 was achieved in 2.0 ± 0.2% yield (decay corrected to start of synthesis) by carbon-11 carbon monoxide aminocarbonylation in 40 min after end of bombardment. In vitro autoradiography with [11C]5 on rat brain sections demonstrated high specific binding, but also strong off-target binding. Ex vivo, only intact tracer was observed in blood plasma at 90 min post injection in healthy rats. PET scanning results demonstrated negligible brain uptake under baseline conditions and this brain uptake did not increase by blocking of efflux transporters using Tariquidar. To conclude, [11C]5 was successfully synthesized and evaluated in healthy rats. However, the inability of [11C]5 to cross the blood-brain-barrier excludes its use for imaging of CSF-1R expression in the brain.

9H-PYRROLO-DIPYRIDINE DERIVATIVES

The invention relates to 9H-pyrrolo-dipyridine derivatives of formula I, processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates.

4, 6-DISUBSTITUTED 2-AMINO-PYRIMIDINES AS HISTAMINE H4 RECEPTOR MODULATORS

The present invention relates to substituted heterocyclic compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.