144291-47-4

Usage

Uses

Methyl 2-(4-Formylphenyl)benzoate is a useful synthetic compound.

Upstream product

• 67-56-1 methanol 
• 88-67-5 2-Iodobenzoic acid 
• 87199-17-5 4-formylphenylboronic acid, 
• 610-94-6 2-bromobenzoic acid methyl ester 
• 610-97-9 o-iodo-methyl-benzoic acid 
• 88-65-3 2-bromobenzoic-acid 
• 114772-38-2 Methyl 4'-(bromomethyl)biphenyl-2-carboxylate 

Downstream Products

• 868555-43-5 methyl 4′-((phenylamino)methyl)[1,1′-biphenyl]-2-carboxylate 
• 868555-41-3 methyl 4′-((benzylamino)methyl)[1,1′-biphenyl]-2-carboxylate 
• 158144-55-9 methyl 4'-(hydroxymethyl)biphenyl-2-carboxylate 

Relevant academic research and scientific papers

Poly(ethylene glycol) supported liquid phase synthesis of biaryls

The liquid phase synthesis of biaiyls via Suzuki cross-coupling reaction on polyethylene glycol) supports (PEGs) is described. The reaction is exemplified by parallel coupling of polymer bound aryl halides with boronic acids. Four different PEGs were employed as soluble polymer supports for parallel synthesis. The generated libraries include both sterically hindered aryl halides (2b, 2d) and boronic acids. The reactions were run in the homogeneous phase and the synthetic sequences performed in parallel fashion. Quantitative conversion in the Suzuki couplings was verified by 1H-NMR analysis (3a-r). The polymer bound products were isolated in good to excellent (52% to 98%) yields by either simple precipitation of the soluble support or column filtration.

First Structure-Activity Relationship Study of Potent BLT2 Agonists as Potential Wound-Healing Promoters

The first potent leukotriene B4 (LTB4) receptor type 2 (BLT2) agonists, endogenous 12(S)-hydroxyheptadeca-5Z,8E,10E-trienoic acid (12-HHT), and synthetic CAY10583 (CAY) have been recently described to accelerate wound healing by enhanced keratinocyte migration and indirect stimulation of fibroblast activity in diabetic rats. CAY represents a very valuable starting point for the development of novel wound-healing promoters. In this work, the first structure-activity relationship study for CAY scaffold-based BLT2 agonists is presented. The newly prepared derivatives showed promising in vitro wound-healing activity.

Discovery of ONO-7300243 from a Novel Class of Lysophosphatidic Acid Receptor 1 Antagonists: From Hit to Lead

Lysophosphatidic acid (LPA) evokes various physiological responses through a series of G protein-coupled receptors known as LPA1-6. A high throughput screen against LPA1 gave compound 7a as a hit. The subsequent optimization of 7a led to ONO-7300243 (17a) as a novel, potent LPA1 antagonist, which showed good efficacy in vivo. The oral dosing of 17a at 30 mg/kg led to reduced intraurethral pressure in rats. Notably, this compound was equal in potency to the α1 adrenoceptor antagonist tamsulosin, which is used in clinical practice to treat dysuria with benign prostatic hyperplasia (BPH). In contrast to tamsulosin, compound 17a had no impact on the mean blood pressure at this dose. These results suggest that LPA1 antagonists could be used to treat BPH without affecting the blood pressure. Herein, we report the hit-to-lead optimization of a unique series of LPA1 antagonists and their in vivo efficacy.

NOVEL BIPHENYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING INFLAMMATORY DISEASES OR AUTOIMMUNE DISEASES COMPRISING THE SAME AS ACTIVE INGREDIENT

The present invention relates to a novel biphenyl derivative or a pharmaceutically acceptable salt thereof, a pharmaceutical composition for preventing or treating inflammatory diseases or autoimmune diseases comprising the same as an active ingredient, and methods for treating inflammatory disease or autoimmune diseases with the pharmaceutical composition. Novel biphenyl derivatives according to the present invention promote the phagocytosis of macrophages and inhibit the chemotaxis to exhibit excellent inflammation terminating and anti-inflammatory effects and thus can be effectively used as therapeutic agents for inflammatory diseases or autoimmune diseases.

General and practical carboxyl-group-directed remote C-H oxygenation reactions of arenes

Two methods for remote aromatic C-H oxygenation reactions, have been developed. Method1, the Cu-catalyzed oxygenation reaction, is highly efficient for cyclization of electron-neutral and electron-rich biaryl carboxylic acids into 3,4-benzocoumarins. Method2, the K2S2O 8-mediated oxygenation reaction, is more general and practical for cyclization of substrates with electron-donating and -withdrawing groups (see scheme). Copyright

The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor

Optimisation of urea (5), identified from high throughput screening and subsequent array chemistry, has resulted in the identification of pyridine carboxamide (33) which is a potent motilin receptor agonist possessing favourable physicochemical and ADME profiles. Compound (33) has demonstrated prokinetic-like activity both in vitro and in vivo in the rabbit and therefore represents a promising novel small molecule motilin receptor agonist for further evaluation as a gastroprokinetic agent.

NOVEL BLT2-MEDIATED DISEASE, AND BLT2 BINDING AGENT AND COMPOUND

[PROBLEM] The compound that selectively binds to BLT2 and the preventive and/or therapeutic drug for BLT2-mediated disease such as skin disease are needed. [MEANS FOR SOLVING THE PROBLEMS] The present invention provides the compound with BLT2 binding activity, salt thereof, solvate thereof or prodrug thereof. Since the compound with BLT2 binding activity, particularly the compound represented by the formula (I) , salt thereof, solvate thereof or prodrug thereof (symbols in formula have the same meanings as specification.) have BLT2 binding activity, it is useful for prevention and/or therapy of BLT2 mediated diseases, e.g., dermatosis, intestinal disease, HIV infection, acquired immunodeficiency syndrome, rejection to transplant, transplant rejection, graft-versus-host disease, autoimmune disease, allergic disease, inflammation, infection, ulcers, lymphoma, malignant tumor, leucaemia, arterial sclerosis, hepatitis, hepatic cirrhosis or cancer, etc.

REMEDY FOR CHRONIC DISEASE

A remedy and/or a preventive for a chronic disease which contains an EDG-2 antagonist. Because of binding to a subtype EDG-2 of LPA receptor, an EDG-2 antagonist is useful in treating and/or preventing chronic diseases (for example, diseases caused by the

LPA RECEPTOR ANTAGONISTS

A compound of the general formula (1): (wherein the symbols are as defined in the description), or a non-toxic salt thereof. This compound engages in LPA receptor bonding and antagonism and hence is useful in the prevention and/or treatment of urinary system disease (symptom with prostatic hypertrophy or neurogenic bladder dysfunction disease, symptom to be caused by spinal cord neoplasm, nucleous hernia, spinal canal stenosis or diabetes, occlusion disease of lower urinary tract, inflammatory disease of lower urinary tract, polyuria), carcinoma-associated disease (solid tumor, solid tumor metastasis, angiofibroma, myeloma, multiple myeloma, Kaposi's sarcoma, leucemia and carcinomatous infiltration transition), proliferative disease (disorder with aberrant angiogenesis, artery obstruction and pulmonary fibrosis), inflammation / immune system disease (psoriasis, nephropathy, hepatitis and pneumonitis symptom), disease caused by secretory dysfunction (Sjogren syndrome), brain-related disease (brain infarction, cerebral apoplexy and brain or peripheral neuropathy) or chronic disease (chronic asthma, glomerulonephritis, obesity, prostate hyperplasia, diseases caused by arteriosclerosis process, rheumatism or atopic dermatitis).

A new precatalyst for the Suzuki reaction - A pyridyl-bridged dinuclear palladium complex as a source of mono-ligated palladiuin(0)

A dinuclear pyridyl-bridged palladium complex, trans-(P,N)-[PdBr(μ- C5H4N-C2,N)(PPh3)]2 1, was obtained from material isolated from the Suzuki cross-coupling reaction of 2-bromopyridine with 2,4-difluorophenylboronic acid in the presence of catalytic (PPh3)4Pd. Complex 1 is an effective precatalyst for the Suzuki cross-coupling reactions of a variety organoboronic acids and aryl bromides, and represents a useful source of mono-ligated palladium(0), "(Ph3P)Pd(0)".