95360-33-1

Usage

Uses

Used in Pharmaceutical Industry:
4-(Chloromethyl)-phenylacetic acid methyl ester is used as a key intermediate in the synthesis of flavonoids, which are a class of compounds with diverse biological activities. Specifically, it is utilized in the production of aromatase inhibitors, a type of drug that helps regulate hormone levels and is used in the treatment of conditions such as breast cancer.
Used in Chemical Synthesis:
As a building block compound, 4-(Chloromethyl)-phenylacetic acid methyl ester is also employed in the synthesis of other complex organic molecules and pharmaceutical agents. Its versatile structure allows for further functionalization and modification, making it a valuable component in the development of new drugs and bioactive compounds.

Upstream product

• 4385-35-7 isochroman-3-one 
• 67-56-1 methanol 
• 6772-67-4 2-chloromethylphenylacetyl chloride 
• 95335-46-9 2-chloromethylphenylacetic acid 

Downstream Products

• 278611-07-7 methyl 2-(2-chloromethylphenyl)-3-hydroxyacrylate 
• 187327-30-6 2-[6-(trifluoromethyl)-2-pyridyloxymethyl]phenylacetic acid methyl ester 
• 278611-08-8 methyl 2-(2-chloromethyl phenyl)-3,3-dimethoxypropionate 
• 117428-95-2 methyl 2-(2'-chloromethylphenyl)-3-methoxyacrylate 

Relevant academic research and scientific papers

Method for preparing 2-(6-trifluoromethylpyridine-2-yloxymethyl) methyl phenylacetate

The invention provides a method for preparing methyl 2-(6-trifluoromethylpyridine-2-yloxymethyl) phenylacetate, and belongs to the technical field of preparation of pesticide intermediates. The preparation method comprises the following steps: by taking 3

Preparation method of picoxystrobin intermediate 2-(2-chloromethyl phenyl)-3-methyl methoxyacrylate

The invention relates to the field of organic synthesis, in particular to a preparation method of picoxystrobin intermediate 2-(2-chloromethyl phenyl)-3-methyl methoxyacrylate. The preparation methodincludes: subjecting 3-isochromanone serving as the raw

Discovery of the First Potent, Selective, and Orally Bioavailable Signal Peptide Peptidase-Like 2a (SPPL2a) Inhibitor Displaying Pronounced Immunomodulatory Effects in Vivo

Signal peptide peptidase-like 2a (SPPL2a) is an aspartic intramembrane protease which has recently been shown to play an important role in the development and function of antigen presenting cells such as B lymphocytes and dendritic cells. In this paper, we describe the discovery of the first selective and orally active SPPL2a inhibitor (S)-2-cyclopropyl-N1-((S)-5,11-dioxo-10,11-dihydro-1H,3H,5H-spiro[benzo[d]pyrazolo[1,2-a][1,2]diazepine-2,1′-cyclopropan]-10-yl)-N4-(5-fluoro-2-methylpyridin-3-yl)succinamide 40 (SPL-707). This compound shows adequate selectivity against the closely related enzymes γ-secretase and SPP and a good pharmacokinetic profile in mouse and rat. Compound 40 significantly inhibited processing of the SPPL2a substrate CD74/p8 fragment in rodents at doses ≤10 mg/kg b.i.d. po. Oral dosing of 40 for 11 days at ≥10 mg/kg b.i.d. recapitulated the phenotype seen in Sppl2a knockout (ko) and ENU mutant mice (reduced number of specific B cells and myeloid dendritic cells). Thus, we believe that SPPL2a represents an interesting and druggable pharmacological target, potentially providing a novel approach for the treatment of autoimmune diseases by targeting B cells and dendritic cells.

Flavonoid aromatizing enzyme inhibitor as well as preparation method and application thereof

The invention relates to a flavonoid aromatizing enzyme inhibitor. Through cyanomethylation reaction and alkylation reaction, some substituted groups on the mother ring of a flavonoid compound are changed and a series of flavonoid compounds and derivatives thereof are synthesized. The structural general formula can be shown in the general formula in claims. In the structural general formula, R1 isselected from any one of -OH or -H, R2 is selected from any one of -H, -OCH3 or -OH, R3 is selected from any one of -H, -OH, -OCH2CN or -OCH3, R4 is selected from any one of -H, -OH, -CH2Ph or -2-(2-methoxy-2-oxo ethyl)benzyloxy, R5 is selected from any one of -H, -OCH2Ph or -OCH3, and R6 is selected from any one of -H, -OH or -OCH3. The flavonoid compounds have good inhibition effect on aromatizing enzyme; through activity test, the maximal value IC50 of inhibiting the activity of the aromatizing enzyme by the inhibitor is equal to 0.251 [mu]mol/L.

NOVEL CRYSTALLINE FORM OF PICOXYSTROBIN, METHOD OF PREPARING AND USE OF THE SAME

A novel crystalline form of the compound of formula (I) (picoxystrobin) is provided. The novel crystalline form of picoxystrobin may be prepared by crystallization from solution in a suitable solvent. Fungicidal compositions comprising the novel crystalline form, a method for controlling fungal infestations at a locus and a use of the novel crystalline form are also provided.

AMINOMETHYL-BIARYL DERIVATIVES AS COMPLEMENT FACTOR D INHIBITORS AND USES THEREOF

The present invention provides a compound of formula (I), a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical com

Syntheses and QSAR studies of benzylimidazole derivatives and benzylcarbazole as potential aromatase inhibitors

In this study, in order to explore new structures and chemical entities as aromatase inhibitors, benzylcarbazole, 12 benzylimidazole derivatives with different substituents on both phenyl and imidazole rings were synthesized and their aromatase inhibitory were evaluated with fluorescent substrate detection method. The results showed that the compounds with carboxyl and ester groups in phenyl ring show better inhibitory activity. The introduction of alkyl groups in imidazole may improve the aromatase inhibitory activity. Most of the compounds were more potent than aminoglutethimide and tamoxifen. 2-[2-{(2-ethyl-4-methyl- 1H-imidazol-1-yl)methyl}phenyl]acetic acid and benzylcarbazole have the highest bioactivities with IC50 values of 6.19 μM and 2.72 μM respectively. A meaningful QSAR model with LOF = 0.00359, R2 = 0.9914, Adj-R 2 = 0.9853, R2cv = 0.9639, F = 161.8, was constructed with genetic functional algorithm using discovery studio 2.1 package.

Synthesis of the phenylpyridal scaffold as a helical peptide mimetic

Phenylpyridal- and phenyldipyridal-based scaffolds have been designed and synthesized as novel helical peptide mimetics. The synthesis required optimisation and selective alkylation in producing 2,6-functionalized 3-hydroxypyridine derivatives for a convergent scheme. The pyridine analogues were coupled by a series of Suzuki/Stille types cross-coupling reactions. A series of biaryl and ter-aryl substituted heterocycles were produced. The synthetic approach was concise and high yielding allowing large variability at the wanted sidechain attachment points. A number of compounds were synthesised to show the versatility of the strategy.

CONSTRAINED COMPOUNDS AS CGRP-RECEPTOR ANTAGONISTS

The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.

SPIRO IMIDAZOLE DERIVATIVES AS PPAR MODULATORS

The invention provides compounds (Ia), (Ib) and (Ic), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated