78775-11-8

Usage

Uses

4-Bromo-3-methylbenzaldehyde can be involved in determining conformational landscape of σ and π coupling Using para-phenylene and "Aviram-Ratner" bridges. Tetrahydroquinoline derivatives as opioid receptor antagonists.

Upstream product

• 41963-20-6 4-bromo-3-methylbenzonirtile 
• 75-17-2 formaldoxime 
• 6933-10-4 amino-5-bromo-2-toluene 
• 7697-28-1 4-bromo-3-methylbenzoic acid 
• 583-70-0 1-bromo-2,4-dimethylbenzene 
• 108-38-3 m-xylene 
• 537-92-8 3-Methylacetanilide 
• 148547-19-7 4-Bromo-3-methylbenzoic acid methyl ester 
• 149104-89-2 4-bromo-3-methylbenzylalcohol 

Downstream Products

• 146308-28-3 2-(4'-bromo-3'-methylphenyl)-5,5-dimethyl-1,3-dioxane 
• 90772-60-4 4-Brom-3-methyl-zimtsaeure 
• 905281-17-6 methyl (2Z)-2-[(benzyloxy)carbonyl]amino-3-(4-bromo-3-methylphenyl)acrylate 
• 73206-52-7 2-methyl-4-isobutylphenyl bromide 
• 75986-23-1 3-Methyl-4-(pyridin-3-ylhydroxymethyl)benzaldehyde 
• 75986-62-8 (E)-2-methyl-3-[3-methyl-4-(pyridin-3-ylmethyl)phenyl]acrylic acid ethyl ester 
• 75986-40-2 (E)-2-methyl-3-[3-methyl-4-(pyridin-3-ylhydroxymethyl)phenyl]acrylic acid ethyl ester 
• 75987-39-2 (E)-3-<4-(3-pyridylmethyl)-3-methylphenyl>-2-methylacrylic acid 
• 877064-90-9 methyl (E)-3-(4-bromo-3-methylphenyl)acrylate 

Relevant academic research and scientific papers

Fluorine thramine intermediate and method for preparing flumbine by using same

The invention discloses a fluororesonide intermediate and a method for preparing the same, and a fluororesonide intermediate -5. Routes include the use of m-xylene as starting materials, halogenation. Oxidation reaction The intermediate -5 is further obtained by hydroximation, cyanolation, hydrolysis reaction or cyanation, oximation, and hydrolysis reaction. As some examples of the present invention, synthetic routes were increased 2 steps from 5 steps in the prior art, but surprisingly high overall yields were obtained and the purity of intermediate -5 was significantly increased. , The starting material of the intermediate -5 is prepared from high 4 - bromo -2 - methylbenzoic acid to low-priced m-xylene, so that the cost of the intermediate -5 is greatly reduced. , The reaction condition is mild, the synthesis difficulty is low, and the environment is more environmentally friendly.

A substituted benzamide isoxazoline derivative or a salt thereof as a pesticidally acceptable salt. Composition and use thereof

The invention belongs to the field of pesticides, and particularly relates to a substituted benzamide isoxazoline derivative or a salt, composition and application thereof as a pesticide acceptable salt, and the compound has the structure of the formula (

Synthesis and Evaluation of PPARδAgonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis

We synthesized a directed library of compounds to explore the structure-activity relationships of peroxisome proliferator-activated receptor δ(PPARδ) activation relative to mesenchymal stem cell (MSC) osteogenesis. Our scaffold used para-substituted cinnamic acids as a polar headgroup, a heteroatom and heterocycle core connecting units, and substituted phenyl groups for the lipophilic tail. Compounds were screened for their ability to increase osteogenesis in MSCs, and the most promising were examined for subunit specificity using a quantitative PPAR transactivation assay. Six compounds were selected for in vivo studies in an ovariectomized mouse model of human postmenopausal osteoporosis. Four compounds improved bone density in vivo, with two (12d and 31a) having activity comparable to that of GW0742, a well-studied PPARδ-selective agonist. 31a (2-methyl-4-[N-methyl-N-[5-methylene-4-methyl-2-[4-(trifluoromethyl)phenyl]thiazole]]aminocinnamic acid) had the highest selectivity for PPARδcompared to other subtypes, its selectivity far exceeding that of GW0742. Our results confirm that PPARδis a new drug target for possible treatment of osteoporosis via in situ manipulation of MSCs.

SELECTIVE FLUORESCENT PROBE FOR ALDEHYDE DEHYDROGENASE

High aldehyde dehydrogenase 1A1 (ALDH1A1) activity has emerged as a reliable marker for the identification of both normal and cancer stem cells. Herein, is presented AlDeSense, a turn-on green fluorescent probe for aldehyde dehydrogenase 1A1 (ALDH1A1) and Ctrl-AlDeSense, a matching non-responsive reagent. AlDeSense exhibits a 20-fold fluorescent enhancement when treated with ALDH1A1. Through the application of surface marker antibody staining, tumorsphere assays, and assessment of tumorigenicity, the disclosed results show that cells exhibiting high AlDeSense signal intensity have properties of cancer stem cells. Herein, is also reported the development of a red congener, red-AlDeSense. Importantly, red-AlDeSense represents one of only a few examples of a turn-on sensor in the red region using the d-PeT quenching mechanism.

As opioid receptor antagonists or inverse agonists of the novel compounds

Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.

A one-pot allylation-hydrostannation sequence with recycling of the intermediate tin waste

A one-pot allylation and hydrostannation of alkynals where the tin byproduct formed in the first step of the reaction is recycled and used in the second step of the sequence is presented. Specifically, a BF3· OEt2-promoted allylstannation of the aldehyde moiety in the alkynal is followed by the introduction of polymethylhydrosiloxane (PMHS) and catalytic B(C6F5)3, which convert the tin byproduct of the allylation into Bu3SnH, which then hydrostannates the alkyne in the molecule. 119Sn and 11B NMR data suggest an organotin fluoride species is formed during the allylation step and involved in the tin recycling step.

BORON-CONTAINING SMALL MOLECULES

This invention provides novel compounds, methods of using the compounds, and pharmaceutical formulations comprising the compounds.

Synthesis and evaluation of 1,2,4-methyltriazines as mGluR5 antagonists

In previous studies we showed that 3-(substituted phenylethynyl)-5- methyl[1,2,4]triazine analogues of MPEP were potent antagonists of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro efficacy assay. In the present study we report

Discovery of GSK1070916, a potent and selective inhibitor of aurora B/C kinase

The Aurora kinases play critical roles in the regulation of mitosis and are frequently overexpressed or amplified in human tumors. Selective inhibitors may provide a new therapy for the treatment of tumors with Aurora kinase amplification. Herein we describe our lead optimization efforts within a 7-azaindole-based series culminating in the identification of GSK1070916 (17k). Key to the advancement of the series was the introduction of a 2-aryl group containing a basic amine onto the azaindole leading to significantly improved cellular activity. Compound 17k is a potent and selective ATP-competitive inhibitor of Aurora B and C with Ki* values of 0.38 ± 0.29 and 1.5 ± 0.4 nM, respectively, and is >250-fold selective over Aurora A. Biochemical characterization revealed that compound 17k has an extremely slow dissociation half-life from Aurora B (>480 min), distinguishing it from clinical compounds 1 and 2. In vitro treatment of A549 human lung cancer cells with compound 17k results in a potent antiproliferative effect (EC50 = 7 nM). Intraperitoneal administration of 17k in mice bearing human tumor xenografts leads to inhibition of histone H3 phosphorylation at serine 10 in human colon cancer (Colo205) and tumor regression in human leukemia (HL-60). Compound 17k is being progressed to human clinical trials.

INSCETICIDAL COMPOUNDS

A compound of formula (I): wherein A1, A2, A3, A4, A1', A2', A3', A4', A5', A6', G1, R1, R2,R3,R