321-24-4

Usage

Chemical Properties

Off-white crystals

InChI:InChI=1/C8H6ClFO2/c1-12-5-2-3-6(8(9)11)7(10)4-5/h2-4H,1H3

Upstream product

• 394-42-3 2-fluoro-4-methoxy-benzoic acid 
• 372-20-3 3-fluorophenol 
• 121219-03-2 4-bromo-3-fluorophenol 
• 82380-18-5 2-fluoro-4-hydroxybenzonitrile 
• 65145-13-3 2-fluoro-4-hydroxybenzoic acid 
• 74457-86-6 1-(2-fluoro-4-methoxyphenyl)-1-ethanone 

Downstream Products

• 331-63-5 1-(chloromethyl)-2-fluoro-4-methoxybenzene 
• 1434159-58-6 methyl {4-[(2-fluoro-4-methoxyphenyl)carbonyl]-5-hydroxy-1-(2-methoxyphenyl)-1H-pyrazol-3-yl}acetate 
• 1449688-69-0 C₁₈H₁₁ClFNO₆ 
• 1449688-63-4 C₂₀H₁₅ClFNO₆ 
• 1449688-70-3 C₁₈H₁₁BrFNO₆ 
• 1449688-64-5 C₂₀H₁₅BrFNO₆ 
• 1290181-04-2 3-(2-fluoro-4-methoxyphenyl)-3-oxopropanenitrile 
• 1346699-36-2 5-ethyl-6-[2-(2-fluoro-4-methoxy-phenyl)benzoxazol-6-yl]-4,5-dihydro-2H-pyridazin-3-one 

Relevant academic research and scientific papers

Design and Identification of a GPR40 Full Agonist (SCO-267) Possessing a 2-Carbamoylphenyl Piperidine Moiety

GPR40/FFAR1 is a G-protein-coupled receptor expressed in pancreatic β-cells and enteroendocrine cells. GPR40 activation stimulates secretions of insulin and incretin, both of which are the pivotal regulators of glycemic control. Therefore, a GPR40 agonist

Copper-Mediated Aminoquinoline-Directed Radiofluorination of Aromatic C?H Bonds with K18F

A Cu-mediated ortho-C?H radiofluorination of aromatic carboxylic acids that are protected as 8-aminoquinoline benzamides is described. The method uses K18F and is compatible with a wide range of functional groups. The reaction is showcased in t

BCL-3 INHIBITORS

The present application relates to compounds of any one of Formulae I, Ia, Ib, Ic, Id, Ie, and If. Compounds of Formula (I) have the structure, wherein A, B, Y, Z, R2, R4, R5, R6, Rq and q are as defined herein. The compounds can be used as inhibitors of Bcl-3 and can be used for the treatment of cancer, particularly metastatic cancer.

Studies on phenothiazines: New microtubule-interacting compounds with phenothiazine A-ring as potent antineoplastic agents

New phenothiazine derivatives 6-20 have been designed, synthesized and evaluated in vitro for their ability to inhibit tubulin polymerization and antiproliferative activity against 60 cancer cell lines, including several multi-drug resistant (MDR) tumor cell lines. The phenothiazine unit may successfully replace the classical 3,4,5-trimethoxyphenyle A ring of parent combretastatin A-4 or phenstatin, confirming previous studies. The most promising structural modulations have been realized on the B ring, the 2′-fluoro-4′-methoxy substitution in compound 6 and the 2′-trifluoromethyl-4′-methoxy substitution in compound 7 providing the best antitubulin and antitumor activity in the current study. Compounds 6-8 and 16 exhibited more important cell growth inhibition than parent phenstatin 2 on human colon Duke's type D, colorectal adenocarcinoma COLO 205 and on human kidney adenocarcinoma A498 cell lines. 10-Methylphenothiazine derivatives 19 and 20 did not show biological activity but exerted bright fluorescence and solvatochromism effects. These molecules deserve further chemical efforts in order to provide valuable tools for biophysical studies.

AROMATIC COMPOUND

Provided is a novel aromatic ring compound having a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula: wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity and a GLP-1 secretagogue action, is useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and affords superior efficacy.

Site-Selective Silylation of Aliphatic C-H Bonds Mediated by [1,5]-Hydrogen Transfer: Synthesis of α-Sila Benzamides

The first example of site-selective silylation of C(sp3)-H bonds mediated by a [1,5]-hydrogen transfer is reported. This reaction occurs selectively at the α-position of benzamides with a combination of tert-butylmagnesium chloride and a catalytic amount of 4,4′-di-tert-butylbipyridine (dtbpy) ligand and provides a facile route for the creation of biologically interesting α-sila benzamides. Late-stage functionalization of the incorporated silyl moieties facilitates the synthesis of N-formyl, cis-enamine, β-hydroxyl, amino, and pyrrole-containing derivatives.

The flocculated acryloyldimethyltauric molecule ligand

Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.

Preparation method of 1-alkyl-2-phenyl-4-quinolones

Provided is a novel method for synthesizing 1-alkyl-2-phenyl-4-quinolones from 2-halobenzoates. The synthesizing method in the present invention has advantages capable of synthesizing 1-alkyl-2-phenyl-4-quinolones in high yield through a simplified stage in a simple reaction condition by means of 2-halobenzoates as an inexpensive starting material.COPYRIGHT KIPO 2015

Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia

A series of 6-acylureido derivatives containing a 3-(pyrrol-2- ylmethylidene)indolin-2-one scaffold were synthesized as potential dual Aurora B/FLT3 inhibitors by replacing the 6-arylureido moiety in 6-arylureidoindolin-2- one-based multi-kinase inhibitors. (Z)-N-(2-(pyrrolidin-1-yl)ethyl)-5-((6-(3-(2- fluoro-4-methoxybenzoyl)ureido)-2-oxoindolin-3-ylidene)methyl)-2, 4-dimethyl-1H-pyrrole-3-carboxamide (54) was identified as a dual Aurora B/FLT3 inhibitor (IC50 = 0.4 nM and 0.5 nM, respectively). Compound 54 also exhibited potent cytotoxicity with single-digit nanomolar IC50 values against the FLT3 mutant-associated human acute myeloid leukemia (AML) cell lines MV4-11 (FLT3-ITD) and MOLM-13 (FLT3-ITD). Compound 54 also specifically induced extrinsic apoptosis by inhibiting the phosphorylation of the Aurora B and FLT3 pathways in MOLM-13 cells. Compound 54 had a moderate pharmacokinetic profile. The mesylate salt of 54 efficiently inhibited tumor growth and reduced the mortality of BALB/c nude mice (subcutaneous xenograft model) that had been implanted with AML MOLM-13 cells. Compound 54 is more potent than sunitinib not only against FLT3-WT AML cells but also active against sunitinib-resistant FLT3-ITD AML cells. This study demonstrates the significance of dual Aurora B/FLT3 inhibitors for the development of potential agents to treat AML.

Nadph oxidase 4 inhibitors and use thereof

The present invention is related to Nox4 inhibitors, pharmaceutical composition thereof and to their use for the treatment and/or prevention of osteoporosis or an osteoclastogenesis dysfunction, in particular osteoporotic and pre-osteoporotic osteoclastog