908600-87-3

Upstream product

• 399-51-9 6-fluoro-1H-indole 
• 13154-24-0 triisopropylsilyl chloride 

Downstream Products

• 908600-73-7 6-fluoroindole-5-carboxylic acid 
• 908600-71-5 6-fluoro-1H-indole-4-carboxylic acid 
• 885520-49-0 6-fluoro-4-iodoindole 

Relevant academic research and scientific papers

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 N-Alkyl-4-(6-fluoro-1H-indol-3-yl)benzamide Derivatives as Anticancer Agents: Design, Synthesis, Biological Evaluation, and Molecular Docking Study

Abstract: A number of novel N-alkyl-4-(6-fluoro-1H-indol-3-yl)benzamide derivatives were synthesized andcharacterized with modern spectroscopic techniques (NMR, IR, and MS). Thesynthesized compounds were assessed for their cytotoxic activities against twocancer cell lines, namely HeLa (cervical cancer) and MCF-7 (breast cancer), byMTT assay. The results showed that the compounds with 3-fluorobenzyl,4-fluorobenzyl, 4-(trifluoromethyl)benzyl, and 4-(diethylamino)butan-2-ylsubstituents on the amide nitrogen atom possess potent activity against bothcancer cell lines. The N-[4-(diethylamino)butan-2-yl]benzamide derivative showed potentialcytotoxic action on HeLa and MCF-7 cell lines with IC50values of 16.07 and 15.84 μg/mL, respectively, which are comparable with thoseof the standard drug doxorubicin. Molecular docking study of these fourcompounds also showed strong binding activity through hydrophobic interactionswith Pin1 protein (PDBID: 2XPB).

4-Substituted Pyrrolo[2,3-d]pyrimidine Compound and Use Thereof

The invention relates to a 4-substituted pyrrolo[2,3-d]pyrimidine compound and the use thereof in preparing medications for treating JAK-targeted diseases such as rheumatoid, immune system diseases, and tumor. The 4-substituted pyrrolo[2,3-d]pyrimidine compound of the invention is as shown in chemical formula I. The activity experimental results of the invention show that the new compound has obvious effect and activity in inhibition of Janus kinases, JAK-STAT, cell proliferation of human lymphocytoma, and rheumatoid arthritis.

TRICYCLIC SULFONAMIDE DERIVATIVES

The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of pain.

TRICYCLIC SULFONAMIDE DERIVATIVES

The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of pain.

ANTIDIABETIC TRICYCLIC COMPOUNDS

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR 40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds may be useful in the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

PYRAZOLOPYRIDINE DERIVATIVES AS ANTICANCER AGENT

The present invention concerns compounds of following general formula (I): (Formula I) and their pharmaceutically acceptable salts, their method of preparation and their uses, notably as anticancer agent.

In search of simplicity and flexibility: A rational access to twelve fluoroindolecarboxylic acids

All twelve indolecarboxylic acids 1-12 carrying both a fluorine substituent and a carboxy group at the benzo ring have been prepared either directly from the corresponding fluoroindoles 13-16 or from the chlorinated derivatives 22, 23 and 25 by hydrogen/metal permutation ("metalation"), or from the bromo- or iodofluoroindoles 17-20 and 26, 27, 29 and 30 by halogen/metal permutation, the organometallic intermediate being each time trapped with carbon dioxide. In most, though not all cases, the nitrogen atom in the five-membered ring had to be protected by a trialkylsilyl group. Some of the bromo- or iodofluoroindoles (26 and 27) were successfully subjected to a basicity gradient-driven selective migration of the heavy halogen. An unexpected finding on the way to the target compounds were the rigorously site-selective metalation of the 5-fluoro-N-(trialkylsilyl)indole (14b; exclusive deprotonation of the 4-position). The fluoroindoles 13-16, although previously known, were accessed more conveniently from suitably substituted nitrobenzenes using the Bartoli or the Leimgruber-Batcho method. A new and very attractive indole synthesis was elaborated consisting of the ortho-lithiation of an N-acyl-protected aniline followed by ortho-formylation, Wittig chloromethylenation and base-catalyzed cyclization accompanied by dehydrochlorination. These five consecutive steps can be contracted to a convenient one-pot protocol. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.