85231-15-8

Usage

Uses

4-Hydroxy-2,5-dimethylbenzaldehyde

Upstream product

• 95-87-4 2,5-Dimethylphenol 
• 74-90-8 hydrogen cyanide 
• 67-66-3 chloroform 
• 93-61-8 N-methyl-N-phenylformamide 
• 16819-05-9 N-<(4-Hydroxy-3,6-dimethyl-phenyl)-methyl>-dimethylamin 
• 10496-93-2 4-Hydroxy-2,5-dimethylbenzenemethanol 
• 7446-70-0 aluminium trichloride 
• 71-43-2 benzene 
• 6745-75-1 2,5-dimethyl-p-anisaldehyde 
• 4885-02-3 Dichloromethyl methyl ether 
• 20524-86-1 dichloromethyl ether 
• 95-78-3 2,5-Dimethylaniline 
• 576-26-1 2.6-dimethylphenol 
• 60431-06-3 1-<(4-Hydroxy-3,5-dimethyl-phenyl)-methyl>-pyrrolidin 

Downstream Products

• 496-78-6 2,4,5-trimethylphenol 
• 90609-92-0 4-hydroxy-2,5-dimethyl-benzaldehyde-oxime 
• 936712-23-1 2-(4-formyl-2,5-dimethyl-phenoxy)-2-methyl-propionic acid methyl ester 
• 18073-33-1 6-methylellipticine 
• 6745-75-1 2,5-dimethyl-p-anisaldehyde 
• 52670-13-0 2-(4-methoxy-2,5-dimethylphenyl)ethanamine 

Relevant academic research and scientific papers

A transition metal-free approach to a regioselective total synthesis of the natural product derivative 6-methylellipticine, a potent anticancer agent

A transition metal-free and regioselective total synthesis of 6-methylellipticine, a potent anticancer agent, was developed. This synthetic approach mainly involved two key reactions: a direct amination of multi-functional phenol via an alkylation-Smiles

Synthesis method of natural product derivative 6-methylellipticine

The invention relates to a synthesis technology of a natural product derivative, and aims at providing a synthesis method of a natural product derivative 6-methylellipticine. The target molecule 6-methylellipticine is synthesized from a cheap and easily available raw material 2,5-dimethylphenol through formylation, iodination, propylene glycol protection, amidation, methylation, transition metal catalysis-free carbazole preparation, propylene glycol protection removal, reductive amination and acid-catalyzed cyclization. The above whole synthesis route is novel, unique and reasonable, and the 6-methylellipticine is synthesized from the 2,5-dimethylphenol without a transition metal catalyst, wherein the method for transition metal catalysis-free synthesis of key intermediates comprising a compound 5 and a compound 7 have not been reported in literatures. The synthesis method has the advantages of cheap and easily available raw materials, simplicity in operation, greenness, and great reduction of the production cost.

Hit-to-lead evaluation of a novel class of sphingosine 1-phosphate lyase inhibitors

Inhibition of sphingosine-1-phosphate lyase has recently been proposed as a potential treatment option for inflammatory disorders such as multiple sclerosis, rheumatoid arthritis, and inflammatory bowel disease. In this report we describe our hit-to-lead evaluation of the isoxazolecarboxamide 6, a high-throughput screening hit (in vitro IC50 = 1.0 μM, cell IC50 = 1.8 μM), as a novel S1P lyase inhibitor. We were able to establish basic structure-activity relationships around 6 and succeeded in obtaining X-ray structural information which enabled structure-based design. With the discovery of 28, enzyme activity was quickly improved to IC50 = 120 nM and cell potency to IC50 = 230 nM. The main liability in the established isoxazolecarboxamide hit series was determined to be metabolic stability. In particular we identified that future lead-optimization efforts to overcome this problem should focus on blocking the N-dealkylation on the secondary amine.

An expedient synthesis of ellipticine via Suzuki-Miyaura coupling

A simple and efficient total synthesis of ellipticine was developed via the Suzuki-Miyaura coupling of sterically sensitive 2-hydroxybenzeneboronic acid with a multifunctional aryl halide using Pd(OAc)2 as a catalyst and Cu(OAc)2·H2O as an additive in DMSO/H2O as a key step followed by double N-arylation and cyclization.

Novel Phosphinic Acid-Containing Thyromimetics

The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.

COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS

The invention provides compounds, 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 Receptor (PPAR) families.

OXAZOLE AND THIAZOLE PPAR MODULATORS

The invention provides compounds (I) 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 Receptor (PPAR) families, particularly the activity of PPARδ.

COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS

The invention provides compounds, 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 Receptor (PPAR) families.

NOVEL PHOSPHORUS-CONTAINING THYROMIMETICS

The present invention relates to compounds of phosphonic acid containing T3 mimetics, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndromex and diabetes.

4-oxy-substituted phenoxyalkyl carboxylic acid, ester, and alcohol derivatives as antihyper-cholesterolemic and antiatherosclerotic agents

Novel 4-oxy substituted phenoxyalkyl carboxylic acid, ester and alcohol derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.