349-24-6

Upstream product

• 348-54-9 2-Fluoroaniline 
• 302-17-0 chloral hydrate 
• 515-83-3 chloral ethyl hemiacetal 
• 51085-49-5 2-fluoroaniline hydrochloride 
• 75-87-6 chloral 

Downstream Products

• 317-20-4 7-fluoro-1H-indole-2,3-dione 
• 387-44-0 7-fluoro-1H-indole 
• 875003-43-3 7-fluoro-1-methyl-1H-indole-2,3-dione 
• 825-22-9 3-fluoroanthranilic acid 
• 71294-03-6 7-fluoro-1,3-dihydro-indol-2-one 
• 143884-84-8 7-fluoro-1H-indole-2,3-dione 3-oxime 
• 111721-75-6 2-bromo-3-fluoroaniline 
• 132715-70-9 2-Bromo-3-fluorobenzamide 
• 132715-69-6 2-bromo-3-fluoro-benzoic acid 
• 1000339-91-2 2-bromo-3-fluorobenzoyl chloride 
• 953066-90-5 N-(3-chloro-4-fluorophenyl)-8-fluoro-N-((4-methylthiazol-5-yl)methyl)-2-oxo-1,2-dihydroquinoline-4-carboxamide 
• 4001-15-4 2-(carboxymethyl-amino)-3-fluoro-benzoic acid 
• 711-70-6 2-(cyanomethyl-amino)-3-fluoro-benzoic acid 

Relevant academic research and scientific papers

Further Studies on Triazinoindoles as Potential Novel Multitarget-Directed Anti-Alzheimer's Agents

The inadequate clinical efficacy of the present anti-Alzheimer's disease (AD) drugs and their low impact on the progression of Alzheimer's disease in patients have revised the research focus from single targets to multitarget-directed ligands. A novel series of substituted triazinoindole derivatives were obtained by introducing various substituents on the indole ring for the development of multitarget-directed ligands as anti-AD agents. The experimental data indicated that some of these compounds exhibited significant anti-AD properties. Among them, 8-(piperidin-1-yl)-N-(6-(pyrrolidin-1-yl)hexyl)-5H-[1,2,4]triazino[5,6-b]indol-3-amine (60), the most potent cholinesterase inhibitor (AChE, IC50 value of 0.32 μM; BuChE, IC50 value of 0.21 μM), was also found to possess significant self-mediated Aβ1-42 aggregation inhibitory activity (54% at 25 μM concentration). Additionally, compound 60 showed strong antioxidant activity. In the PAMPA assay, compound 60 exhibited blood-brain barrier penetrating ability. An acute toxicity study in rats demonstrated no sign of toxicity at doses up to 2000 mg/kg. Furthermore, compound 60 significantly restored the cognitive deficits in the scopolamine-induced mice model and Aβ1-42-induced rat model. In the in silico ADMET prediction studies, the compound satisfied all the parameters of CNS acting drugs. These results highlighted the potential of compound 60 to be a promising multitarget-directed ligand for the development of potential anti-AD drugs.

Design and development of Isatin-triazole hydrazones as potential inhibitors of microtubule affinity-regulating kinase 4 for the therapeutic management of cell proliferation and metastasis

Microtubule affinity-regulating kinase 4 (MARK4) is a potential drug target as the same is found to be over expressed in several types of cancers. In search of effective MARK4 inhibitors, we have synthesized and characterized Isatin-triazole hydrazones (9a-i) and evaluated their inhibitory potential. Of all the compounds, 9g showed better binding affinity and enzyme inhibition potential in sub micromolar range. Human serum albumin (HSA) binding assay suggested an easy transportation of 9g in blood stream due to its binding affinity. In vitro anticancer studies performed on MCF-7, MDA-MB-435s and HepG2 cells using 9g showed inhibition of cell proliferation and cell migration. Further, 9g induces apoptosis in these cancerous cells, with IC50 values of 6.22, 9.94 and 8.14 μM, respectively. Putatively, 9g seems to cause oxidative stress resulting in apoptosis. Functional assay of 9g with a panel of 26 kinases showed MARK4 specific profile. In conclusion, 9g seems to possess an effective inhibitory potential towards MARK4 adding an additional repertoire to anticancer therapeutics.

Palladium(II)/N-Heterocyclic Carbene Catalyzed One-Pot Sequential α-Arylation/Alkylation: Access to 3,3-Disubstituted Oxindoles

Rationally designed fluorene-based mono- and bimetallic Pd-PEPPSI complexes were synthesized and demonstrated to be effective for the one-pot sequential α-arylation/alkylation of oxindoles. This streamlined approach offers efficient access to functionalized 3,3-disubstituted oxindoles in excellent yields (up to 89%) under mild reaction conditions.

Synthesis of 7-halo indoles (by machine translation)

The present invention relates to synthesis of 7? Halo indole method, comprising the steps of:O-halogenated aniline, chloral hydrate and hydroxylamine hydrochloride by the Sandmeyer reaction to synthesize 7? halogenating isatin ; 7? halogenating isatin dissolved with an organic solvent, in the reducing agent by reduction reaction under the conditions of 7? Halo indole, the reducing agent is an alkali metal borohydride system, four system adopts, lithium hydride system or triethyl silane system. The beneficial effect of the invention is:in order to O-halogenated aniline and the chloral hydrate is, hydroxylamine hydrochloride as raw materials, by the Sandmeyer shall synthesis method for preparing compositions b isonitroso 7? halogenating isatin, and then by further reduction and system reduction to prepare 7? Halo indole; by the 7? Preparation halogenating isatin 7? Halo indole method, the raw material is easy to obtain, low price, higher process yield, the product purity is good, simple operation, and the like, is suitable for batch preparation 7? Halo indole. (by machine translation)

A cinchona alkaloid catalyzed enantioselective sulfa-Michael/aldol cascade reaction of isoindigos: Construction of chiral bispirooxindole tetrahydrothiophenes with vicinal quaternary spirocenters

A cinchona alkaloid catalyzed diastereoselective and enantioselective sulfa-Michael/aldol cascade reaction between 1,4-dithiane-2,5-diol and isoindigos has been successfully developed to afford the highly congested bispirooxindole tetrahydrothiophenes with vicinal quaternary spirocenters in high yields (up to 91%), excellent diastereoselectivities (up to >20 : 1 dr), and good enantioselectivities (up to 98% ee). Some synthetic transformations of the reaction products were also studied.

7-SUBSTITUTED INDIRUBIN-3'OXIMES AND THEIR APPLICATIONS

The invention relates to new 3′-, 7-substituted-indirubins of formula (I) wherein R represents N—OH, N—O-alkyl or N—O—CO-alkyl, NO—(Ra)n1-Het, N—O—(Y)n1—NRaRb, N—O—CO—N(RbRc), ra

QUINOLONES USEFUL AS INDUCIBLE NITRIC OXIDE SYNTHASE INHIBITORS

The present invention relates to novel quinolones of Formula I that inhibit inducible NOS synthase together with methods of synthesizing and using the compounds including methods for inhibiting or modulating nitric oxide synthesis and/or lowering nitric oxide levels in a patient by administering the compounds for the treatment of disease.

Methods and Compositions for Selectin Inhibition

The present teachings relate to novel compounds of formula I: wherein the constituent variables are as defined herein. Compounds of the present teachings can act as antagonists of the mammalian adhesion proteins known as selecting. Methods for treating or preventing selectin-mediated disorders are provided, which include administration of these compounds in a therapeutically effective amount.

Synthesis of insecticidal fluorinated anthranilic diamides

A series of highly active fluorinated anthranilic diamide insecticides have been prepared and their biological activity assessed on two aphid species in the search for systemically active compounds that control Hemiptera. In addition, we have demonstrated a new synthesis of N-aryl 3-fluoropyrazoles.

3′-substituted 7-halogenoindirubins, a new class of cell death inducing agents

Indirubins are kinase inhibitory bis-indoles that can be generated from various plant, mollusk, mammalian, and bacterial sources or chemically synthesized. We here report on the synthesis and biological evaluation of 3′-substituted 7-halogenoindirubins. M