849934-94-7

Usage

Uses

Used in Pharmaceutical Research:
Methyl 2-(4-bromo-2-chlorophenyl)acetate is used as a building block in the synthesis of pharmaceutical drugs. Its unique structure allows for the creation of bioactive molecules with potential therapeutic applications.
Used in Agrochemicals:
In the agrochemical industry, Methyl 2-(4-bromo-2-chlorophenyl)acetate is utilized as an intermediate for the development of various agrochemicals, contributing to the production of effective pest control agents and other agricultural products.
Used in Organic Synthesis:
Methyl 2-(4-bromo-2-chlorophenyl)acetate is employed as a key intermediate in organic synthesis, enabling the creation of a wide range of chemical compounds for various industrial and research applications. Its versatility and reactivity make it an essential component in the synthesis process.

Upstream product

• 67197-54-0 2-(4-bromo-2-chlorophenyl)acetonitrile 
• 916516-89-7 2-(4-bromo-2-chlorophenyl)acetic acid 
• 74-88-4 methyl iodide 
• 89794-02-5 4-bromo-2-chlorotoluene 
• 89720-77-4 4-bromo-1-bromomethyl-2-chlorobenzene 
• 67-56-1 methanol 
• 75-36-5 acetyl chloride 
• 31928-47-9 4-bromo-2-chloroiodobenzene 
• 53429-22-4 methyl 2-bromozincacetate 
• 185315-48-4 (4-bromo-2-chlorophenyl)methanol 
• 59748-90-2 4-Bromo-2-chloro-benzoic Acid 

Downstream Products

• 849934-95-8 methyl 2-(2-chloro-4-(1,1,2,2-tetramethyl-1λ4,2λ4,4-dioxaborolan-4-yl)phenyl)acetate 
• 916516-90-0 2-(4-bromo-2-chlorophenyl)ethyl alcohol 
• 1428761-22-1 methyl 2-(2-chloro-4-(2-methyloxazol-5-yl)phenyl)acetate 
• 1433193-87-3 2-chloro-6-(2-chloro-4-(6-methylpyrazin-2-yl)phenyl)-8-ethylpyrido[2,3-d]pyrimidin-7(8H)-one 
• 1432908-05-8 6-(2-chloro-4-(6-methylpyrazin-2-yl)phenyl)-8-ethyl-2-((2-(1-methylpiperidin-4-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one 

Relevant academic research and scientific papers

PHD INHIBITOR COMPOUNDS, COMPOSITIONS, AND USE

The present invention provides, in part, novel small molecule inhibitors of PHD, having a structure according to Formula (A), and sub-formulas thereof, or a pharmaceutically acceptable salt thereof. The compounds provided herein can be useful for treatmen

Discovery of carboxyl-containing biaryl ureas as potent RORγt inverse agonists

GSK805 (1) is a potent RORγt inverse agonist, but a drawback of 1 is its low solubility, leading to a limited absorption in high doses. We have explored detailed structure-activity relationship on the amide linker, biaryl and arylsulfonyl moieties of 1 trying to improve solubility while maintaining RORγt activity. As a result, a novel series of carboxyl-containing biaryl urea derivatives was discovered as potent RORγt inverse agonists with improved drug-like properties. Compound 3i showed potent RORγt inhibitory activity and subtype selectivity with an IC50 of 63.8 nM in RORγ FRET assay and 85 nM in cell-based RORγ-GAL4 promotor reporter assay. Reasonable inhibitory activity of 3i was also achieved in mouse Th17 cell differentiation assay (76percent inhibition at 0.3 μM). Moreover, 3i had greatly improved aqueous solubility at pH 7.4 compared to 1, exhibited decent mouse PK profile and demonstrated some in vivo efficacy in an imiquimod-induced psoriasis mice model.

BIARYL UREA DERIVATIVE OR SALT THEREOF, AND MANUFACTURING AND APPLICATION OF SAME

The present invention discloses a biaryl urea RORγt inhibitor, and specifically relates to a biaryl urea derivative, as represented by formula I, with an RORγt inhibiting activity, and a preparation process thereof, and a pharmaceutical composition comprising the compound. Further disclosed is use of the compound for treating an RORγt-related disease.

Chemically Diverse Group i p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window

p21-activated kinase 1 (PAK1) has an important role in transducing signals in several oncogenic pathways. The concept of inhibiting this kinase has garnered significant interest over the past decade, particularly for targeting cancers associated with PAK1 amplification. Animal studies with the selective group I PAK (pan-PAK1, 2, 3) inhibitor G-5555 from the pyrido[2,3-d]pyrimidin-7-one class uncovered acute toxicity with a narrow therapeutic window. To attempt mitigating the toxicity, we introduced significant structural changes, culminating in the discovery of the potent pyridone side chain analogue G-9791. Mouse tolerability studies with this compound, other members of this series, and compounds from two structurally distinct classes revealed persistent toxicity and a correlation of minimum toxic concentrations and PAK1/2 mediated cellular potencies. Broad screening of selected PAK inhibitors revealed PAK1, 2, and 3 as the only overlapping targets. Our data suggest acute cardiovascular toxicity resulting from the inhibition of PAK2, which may be enhanced by PAK1 inhibition, and cautions against continued pursuit of pan-group I PAK inhibitors in drug discovery.

An optimized synthesis of the potent and selective Pak1 inhibitor FRAX-1036

FRAX-1036 is a p21-activated kinase I inhibitor of significant interest to cancer biologists yet no commercial providers or detailed procedures are available. In this Letter, we chronicle the optimized synthesis of FRAX-1036, one of the most specific Pak1

TBK/IKK INHIBITOR COMPOUNDS AND USES THEREOF

The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.

2- PYRIDONE COMPOUND

PROBLEM TO BE SOLVED: To provide a compound that has excellent glucokinase (GK) activating action and is useful as a pharmaceutical. SOLUTION: The present invention provides a 2-pyridone compound represented by formula [1], and a tautomer or stereoisomer of the compound, or their pharmacologically acceptable salts, or their solvates (where R1 is RA-ZA-; RA is any of a carboxy group, a sulfo group or formula [5]). COPYRIGHT: (C)2016,JPOandINPIT

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pKa Polar Moiety

Signaling pathways intersecting with the p21-activated kinases (PAKs) play important roles in tumorigenesis and cancer progression. By recognizing that the limitations of FRAX1036 (1) were chiefly associated with the highly basic amine it contained, we devised a mitigation strategy to address several issues such as hERG activity. The 5-amino-1,3-dioxanyl moiety was identified as an effective means of reducing pKa and logP simultaneously. When positioned properly within the scaffold, this group conferred several benefits including potency, pharmacokinetics, and selectivity. Mouse xenograft PK/PD studies were carried out using an advanced compound, G-5555 (12), derived from this approach. These studies concluded that dose-dependent pathway modulation was achievable and paves the way for further in vivo investigations of PAK1 function in cancer and other diseases.

SERINE/THREONINE KINASE INHIBITORS

Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.