39576-83-5

Usage

Uses

Used in Pharmaceutical Industry:
8-METHYL-2,4-DICHLOROQUINAZOLINE is used as a key intermediate for the synthesis of various drugs, targeting a range of medical conditions such as cancer and neurodegenerative diseases. Its unique structure and reactivity contribute to the development of novel therapeutic agents with potential efficacy in treating these conditions.
Used in Agrochemical Industry:
8-METHYL-2,4-DICHLOROQUINAZOLINE is utilized as a building block in the creation of agrochemicals, playing a crucial role in the synthesis of compounds that can be used in agriculture to protect crops from pests and diseases, thereby enhancing crop yield and quality.
Used in Chemical Synthesis:
As a versatile intermediate, 8-METHYL-2,4-DICHLOROQUINAZOLINE is used in the synthesis of more complex organic compounds, contributing to the advancement of organic chemistry and the development of new chemical entities with diverse applications.
Used in Material Science and Technology Development:
8-METHYL-2,4-DICHLOROQUINAZOLINE may also have applications in the development of new materials and technologies, owing to its potential to be integrated into innovative molecular structures and systems that could have wide-ranging uses in various industries.

Upstream product

• 67449-23-4 8-methyl-2,4-dioxo-1,2,3,4-tetrahydroquinazoline 
• 10026-13-8 phosphorus pentachloride 
• 10025-87-3 trichlorophosphate 
• 4389-45-1 3-methylantranilic acid 

Downstream Products

• 62484-40-6 2-chloro-8-methylquinazolin-4(3H)-one 
• 1616709-24-0 2-((5H-pyrrolo[3,4-b]pyridine-6(7H)-yl)methyl)-N-(2,4-dimethoxybenzyl)-7-methyl-[1,2,4]triazolo[1,5-c]quinazolin-5-amine 
• 1616709-23-9 2-(chloromethyl)-N-(2,4-dimethoxybenzyl)-7-methyl-[1,2,4]triazolo[1,5-c]quinazolin-5-amine 
• 1616709-22-8 (5-((2,4-dimethoxybenzyl)amino)-7-methyl-[1,2,4]triazolo[1,5-c]quinazolin-2-yl)methanol 

Relevant academic research and scientific papers

Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer

Tankyrases (TNKS/TNKS2) belong to the poly(ADP-ribose) polymerase family. Inhibition of their enzymatic activities attenuates the Wnt/β-catenin signaling, which plays an important role in cancer pathogenesis. We previously reported the discovery of RK-287107, a spiroindoline-based, highly selective, potent tankyrase inhibitor. Herein we describe the optimization process of RK-287107 leading to RK-582, which exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered. In addition to the dose-dependent elevation and attenuation of the levels of biomarkers AXIN2 and β-catenin, respectively, results of the TCF reporter and cell proliferation studies on COLO-320DM are discussed.

DIACYLGLYCEROL KINASE MODULATING COMPOUNDS

The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.

Synthesis of Novel Hydroxymethyl-Substituted Fused Heterocycles

Examples of hydroxymethylated analogues of heteroaryl cores such as quinazolin-4-ones, isoquinolin-1(2H)-ones, pyrido[3,4-d]pyrimidin-4(3H)-ones, chromen-4-ones and pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones are sparse or non-existent in the scientific literature. We have demonstrated that such compounds are accessible by using standard procedures from readily available raw materials.

BICYCLIC DERIVATIVE CONTAINING PYRIMIDINE RING, AND PREPARATION METHOD THEREFOR

The present invention provides: a bicyclic derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof; a preparation method therefor, a pharmaceutical composition comprising the same; and a use therefor. According to the present invention, the bicyclic compound derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof acts as a 5-HT4 receptor agonist, and thus can be usefully applied to the prevention or treatment of dysfunction in gastrointestinal motility, for example, gastrointestinal diseases such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, diabetic gastric atony and the like.

HETEROCYCLIC COMPOUNDS AS ANTIBIOTIC POTENTIATORS

The invention relates to heterocyclic compounds and their use as antibiotics and/or as antibiotic potentiators. The compounds may act as colistin potentiators and SOS inhibitors.

Pyrimidinone nicotinamide mimetics as selective tankyrase and Wnt pathway inhibitors suitable for in vivo pharmacology

The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ?-catenin, can lead to oncogenesis. Inhibition of the poly(ADP-r

Antileishmanial activity of a series of N2, N 4-disubstituted quinazoline-2,4-diamines

A series of N2,N4-disubstituted quinazoline-2,4- diamines has been synthesized and tested against Leishmania donovani and L. amazonensis intracellular amastigotes. A structure-activity and structure-property relationship study was conducted in part using the Topliss operational scheme to identify new lead compounds. This study led to the identification of quinazolines with EC50 values in the single digit micromolar or high nanomolar range in addition to favorable physicochemical properties. Quinazoline 23 also displayed efficacy in a murine model of visceral leishmaniasis, reducing liver parasitemia by 37% when given by the intraperitoneal route at 15 mg kg-1 day-1 for 5 consecutive days. Their antileishmanial efficacy, ease of synthesis, and favorable physicochemical properties make the N2,N 4-disubstituted quinazoline-2,4-diamine compound series a suitable platform for future development of antileishmanial agents.

Ligand based design of novel histamine H4 receptor antagonists; Fragment optimization and analysis of binding kinetics

The histamine H4 receptor is a G protein-coupled receptor that has attracted much interest for its role in inflammatory and immunomodulatory functions. In our search for new H4R ligands, a low affinity isoquinoline fragment was optimized to 7-(furan-2-yl)-4-(piperazin-1-yl) quinazolin-2-amine (VUF11489), as a new H4R antagonist. Analysis of its binding kinetics at the human H4R showed this compound to have a very different dissociative half-life in comparison with reference antagonist JNJ7777120.

Structure-activity relationship and pharmacokinetic studies of sotrastaurin (aeb071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis

Protein kinase C (PKC) isotypes have emerged as key targets for the blockade of early T-cell activation. Herein, we report on the structure-activity relationship and the detailed physicochemical and in vivo pharmacokinetic properties of sotrastaurin (AEB071, 1), a novel maleimide-based PKC inhibitor currently in phase II clinical trials. Most notably, the preferred uptake of sotrastaurin into lymphoid tissues is an important feature, which is likely to contribute to its in vivo efficacy.

2-AMINOQUINAZOLINE DERIVATIVE

An object of the present invention is to provide compounds which are useful as protein kinase inhibitors. Disclosed is a 2-aminoquinazoline derivative represented by the following formula (I): wherein R1 represents a lower alkyl group which may be substituted with a halogen atom, or a halogen atom; R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted acylamino group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, or a substituted or unsubstituted lower alkylureido group; and X, Y and Z each independently represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group, a cyano group, a carbamoyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted lower alkoxycarbonylamino group, a substituted or unsubstituted lower alkylaminocarbonyl group, a lower alkylsulfonylamino group, a substituted or unsubstituted lower alkylureido group, or a substituted or unsubstituted acylamino group, or X and Y may be combined to form a 5- to 6-membered ring forming a bicyclic fused ring, wherein the 5- to 6-membered ring may optionally have a substituent, provided that when X and Y are not combined to form a fused ring, R2 represents a hydrogen atom and, when X and Y are combined to form a fused ring, a saturated or unsaturated, bicyclic alicyclic or heterocyclic fused ring can be formed.