188186-87-0

Upstream product

• 109-87-5 Dimethoxymethane 
• 6921-66-0 4-chloro-2-hydroxy acetophenone 
• 107-30-2 chloromethyl methyl ether 
• 584-08-7 potassium carbonate 
• 89125-42-8 bromomethylmethyl ether 

Downstream Products

• 188186-90-5 methyl 2-(4-chloro-2-methoxymethoxy)benzoylacetate 

Relevant academic research and scientific papers

Methoxymethylation of substituted alcohols using dimethoxymethane over Mo(VI)/ZrO2

The methoxymethylation reaction of alcohols was studied on Mo/ZrO2 (MZ) catalysts. The catalyst containing 5, 10 and 15 % Mo(VI) ions was prepared by solution combustion method. These solid acid catalytic materials were characterized by NH3- TPD, powder XRD, BET, FTIR spectroscopy, scanning electron microscopy, transmission electron spectroscopy and ICP- OES techniques. These catalysts were evaluated for their catalytic activity in the synthesis of methoxymethylation reactions of various substituted alcohols with dimethoxymethane in shorter reaction times (20 min) at moderate temperature (40 °C) with excellent yields (around 99 %). The main features of the Mo/ZrO2 catalyzed reaction are high yields, ease of scale up to gram scale, recyclable catalysts, inexpensive reagents, ecofriendly catalysts and a solvent free approach for the synthesis of methoxymethylated products.

Synthesis and structure-activity relationships of 2-acylamino-4,6-diphenylpyridine derivatives as novel antagonists of GPR54

GPR54 is a G protein-coupled receptor (GPCR) which was formerly an orphan receptor. Recent functional study of GPR54 revealed that the receptor has an essential role to modulate sex-hormones including GnRH. Though antagonists of GPR54 are expected to be novel drugs for sex-hormone dependent diseases such as prostate cancer or endometriosis, small molecule GPR54 antagonists have not been reported. We have synthesized a series of 2-acylamino-4,6-diphenylpyridines to identify potent GPR54 antagonists. Detailed structure-activity relationship studies led to compound 9l with an IC50 value of 3.7 nM in a GPR54 binding assay, and apparent antagonistic activity in a cellular functional assay.

PYRIDYLPHENOL COMPOUND AND USE THEREOF

The present invention provides a compound which has metastin receptor antagonist activity and is useful for preventing and treating hormone-dependent cancer, benign prostatomegaly, endometriosis, precocious puberty, uterine myoma or the like. More specifically, the present invention provides a compound, represented by the formula: or a salt thereof, a prodrug thereof, and a pharmaceutical agent containing the same; wherein Ring A represents a 5- to 8-membered homocyclic or heterocyclic group optionally having a substituent other than formula -X-R1 wherein X represents a bond or a spacer, and R1 represents optionally substituted amino or an optionally substituted nitrogen-containing heterocyclic group; Ring B represents an optionally substituted benzene ring; R2 represents an optionally substituted homocyclic or heterocyclic group; and R3 and R4 independently represent a hydrogen atom, cyano, acyl or an optionally substituted hydrocarbon group.

ENDOTHELIN RECEPTOR ANTAGONISTS

Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.