1240113-40-9

Usage

Uses

Used in Medicinal Chemistry:
1H-Indole, 4-fluoro-5-iodois used as a building block for the development of new drugs with diverse biological activities. Its unique chemical and physical properties, introduced by the fluorine and iodine atoms, make it a promising candidate for the design and synthesis of pharmaceutical compounds with improved potency, selectivity, and pharmacokinetic properties.
Used in Synthetic Organic Chemistry:
1H-Indole, 4-fluoro-5-iodois used as a target molecule for synthetic organic chemists exploring the synthesis of complex molecules. Its structure and reactivity provide opportunities for the development of novel synthetic routes and methodologies, which can be applied to the preparation of other biologically active compounds and advanced materials.
Used in Drug Discovery and Development:
1H-Indole, 4-fluoro-5-iodois used as a starting material or intermediate in the drug discovery and development process. Its unique properties and reactivity can be leveraged to design and synthesize new drug candidates with potential therapeutic applications in various disease areas, such as cancer, neurological disorders, and infectious diseases.
Used in Radiolabeling and Imaging:
1H-Indole, 4-fluoro-5-iodocan be used as a radiolabeling agent in molecular imaging studies. The presence of the iodine atom allows for the incorporation of radioactive isotopes, such as iodine-125 or iodine-131, which can be used to track the distribution and metabolism of the compound in biological systems. This can provide valuable insights into the pharmacokinetics and pharmacodynamics of the compound and aid in the optimization of drug candidates.
Used in Chemical Synthesis and Modification:
1H-Indole, 4-fluoro-5-iodois used as a versatile building block in chemical synthesis and modification. Its unique functional groups can be further modified or derivatized to generate a variety of new compounds with different properties and applications. This can lead to the discovery of novel chemical entities with improved biological activities and selectivity profiles.

Upstream product

• 908600-85-1 4-fluoro-1-(triisopropylsilyl)-1H-indole 
• 387-43-9 4-fluoroindole 
• 1240113-38-5 (4-fluoro-5-iodo-indol-1-yl)-triisopropylsilane 

Downstream Products

• 288385-89-7 4-fluoro-5-methoxy-1H-indole 

Relevant academic research and scientific papers

Fluorinated indole-imidazole conjugates: Selective orally bioavailable 5-HT7 receptor low-basicity agonists, potential neuropathic painkillers

The 5-HT7 receptor has recently gained much attention due to its involvement in multiple physiological functions and diseases. The insufficient quality of the available molecular probes prompted design of fluorinated 3-(1-alkyl-1H-imidazol-5-yl)-1H-indoles as a new generation of selective 5-HT7 receptor agonists. A potent and drug-like agonist, 3-(1-ethyl-1H-imidazol-5-yl)-5-iodo-4-fluoro-1H-indole (AGH-192, 35, Ki 5-HT7R = 4 nM), was identified by optimizing the halogen bond formation with Ser5.42 as the supposed partner. The compound was characterized by excellent water solubility, high selectivity over related CNS targets, high metabolic stability, oral bioavailability and low cytotoxicity. Rapid absorption into the blood, medium half-life and a high peak concentration in the brain Cmax = 1069 ng/g were found after i.p. (2.5 mg/kg) administration in mice. AGH-192 may thus serve as the long-sought tool compound in the study of 5-HT7 receptor function, as well as a potential analgesic, indicated by the antinociceptive effect observed in a mouse model of neuropathic pain.

IMIDAZOLYL-SUBSTITUTED INDOLE DERIVATIVES BINDING 5-HT7 SEROTONIN RECEPTOR AND PHARMACEUTICAL COMPOSITIONS THEREOF

The invention relates to a new class of substituted indole derivatives that are able to activate 5-HT7 serotonin receptor. These compounds bind 5-HT7 serotonin receptor with high affinity and selectivity, while possessing favourable physicochemical properties. The compounds of the invention are the first described low-basicity 5-HT7 receptor agonists. The invention also relates to use of such compounds in the treatment or prevention of 5-HT7 receptor-related disorders, especially of the central nervous system. The invention also relates to the isotopically labelled compounds for use in the in vivo diagnostics or imaging of a 5-HT7 serotonin receptor.

Radiosynthesis of 4-[18F]fluoro-l-tryptophan by isotopic exchange on carbonyl-activated precursors

Several 18F-labeled aromatic amino acids have been developed primarily for tumor imaging with positron-emission-tomography (PET). Also, 18F-labeled tryptophan derivatives were synthesized by electrophilic 18F-fluorination or by introducing a [18F]fluoroalkyl group. Here, a 3-step method for a nucleophilic radiosynthesis of 4-[18F]fluoro-l-tryptophan was developed. A carbonyl activated precursor containing a chiral amino acid building block was radiofluorinated by isotopic exchange, followed by removal of the activating formyl group by reductive decarbonylation and subsequent cleavage of the building block under acidic conditions. The title compound was obtained within 100 min with a radiochemical yield of about 13%, a molar activity of >70 MBq/mmol and an enantiomeric excess of >99%.

NOVEL COMPOUNDS EFFECTIVE AS XANTHINE OXIDASE INHIBITORS, METHOD FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

The present invention relates to novel compounds which are effective as an inhibitor for xanthine oxidase, a process for preparing the same, and a pharmaceutical composition comprising a therapeutically effective amount of the same.