507263-18-5

Usage

Structure

An ester derivative of 4-(3-methoxyphenyl)-1-piperazinecarboxylic acid

Usage

Commonly used in pharmaceutical research and development

Therapeutic potential

Studied for potential effects on various diseases and conditions, including neurological disorders and psychiatric illnesses

Possible applications

Antipsychotic or antidepressant agent, treatment of other mental health conditions

Synthesis use

May be used as a precursor or intermediate in the synthesis of other pharmaceutical compounds

Upstream product

• 2845-89-8 1-chloro-3-methoxy-benzene 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 2398-37-0 3-methoxyphenyl bromide 
• 24424-99-5 di-tert-butyl dicarbonate 
• 16015-71-7 4-(3-methoxyphenyl)piperazine 

Downstream Products

• 59817-32-2 3-(piperazin-1-yl)phenol 
• 1146950-52-8 tert-butyl 4-(3-methoxyl-4-bromophenyl)piperazine-1-carboxylate 
• 1416634-02-0 C₃₅H₄₀N₄O₅ 
• 1416633-94-7 C₃₄H₃₇ClN₄O₅ 
• 1416633-66-3 C₂₉H₃₈N₄O₃ 

Relevant academic research and scientific papers

Synthesis of fluorescein derivatives containing metal-coordinating heterocycles

Fluorescein derivatives that contain Lewis basic heterocycles have been synthesized by concise reaction sequences. The preparation of these compounds proceeds by functionalization of an electron-rich aromatic precursor and subsequent condensation to form the fluorophore. These compounds are envisioned as components of metal-based sensors.

MONOACYLGLYCEROL LIPASE INHIBITORS

Provided are compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof: Also provided are compositions comprising compounds of formula (I). The compounds and compositions are also provided for use as medicaments, for example as medicaments useful in the treatment of a condition modulated by monoacylglycerol lipase (MAGL). Also provided are the use of compounds and compositions for the inhibition of monoacylglycerol lipase (MAGL).

A class of GPR40 agonist compounds with amide structure, and uses thereof

The present invention relates to a class of amide compounds with a novel structure, and a pharmaceutical composition thereof, wherein the structure of the amide compound is represented by a general formula (I). According to the present invention, the amide compound (I) can regulate GPR40 activity, and can be used for GPR40 activity related diseases such as diabetes and metabolic syndrome. The formula I is defined in the specification.

Identification of novel GLUT inhibitors

The compound class of 1H-pyrazolo[3,4-d]pyrimidines was identified using HTS as very potent inhibitors of facilitated glucose transporter 1 (GLUT1). Extensive structure–activity relationship studies (SAR) of each ring system of the molecular framework was established revealing essential structural motives (i.e., ortho-methoxy substituted benzene, piperazine and pyrimidine). The selectivity against GLUT2 was excellent and initial in vitro and in vivo pharmacokinetic (PK) studies are encouraging.

SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITOR

Disclosed are a 2-aminopyridine derivative having protein kinase inhibition activity, a preparation method and a pharmaceutical composition thereof Also disclosed are uses of the compounds and the pharmaceutical compositions thereof in the preparation of drugs for treating and/or preventing protein kinase-related diseases.

Nitrofuranyl Methyl Piperazines as New Anti-TB Agents: Identification, Validation, Medicinal Chemistry, and PK Studies

Whole-cell screening of 20,000 drug-like small molecules led to the identification of nitrofuranyl methylpiperazines as potent anti-TB agents. In the present study, validation followed by medicinal chemistry has been used to explore the structure-activity relationship. Ten compounds demonstrated potent MIC in the range of 0.17-0.0072 μM against H37Rv Mycobacterium tuberculosis (MTB) and were further investigated against nonreplicating and resistant (RifR and MDR) strains of MTB. These compounds were also tested for cytotoxicity. Among the 10 tested compounds, five showed submicromolar to nanomolar potency against nonreplicating and resistant (RifR and MDR) strains of MTB along with a good safety index. Based on their overall in vitro profiles, the solubility and pharmacokinetic properties of five potent compounds were studied, and two analogues, 14f and 16g, were found to have comparatively better solubility than others tested and acceptable pharmacokinetic properties. This study presents the rediscovery of a nitrofuranyl class of compounds with improved aqueous solubility and acceptable oral PK properties, opening a new direction for further development.

ARYLPIPERAZINE OPIOID RECEPTOR ANTAGONISTS

Provided are opioid receptor antagonists represented by the formula (I) where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.

1-Substituted 4-(3-Hydroxyphenyl)piperazines are pure opioid receptor antagonists

This report describes the discovery that 1-substituted 4-(3-hydroxyphenyl) piperazines are pure opioid receptor antagonists. Compounds in this new series include N-phenylpropyl (3S)-3-methyl-4-(3-hydroxyphenyl)piperazine and (3R)-3-methyl-4-(3-hydroxyphenyl)piperazine, both of which display low nanomolar potencies at μ, δ, and κ receptors and pure antagonist properties in a [35S]GTPγS assay.

PYRIDINE AND PYRAZINE DERIVATIVES - 083

The invention concerns pyridine and pyrazine derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of W, G1, G2, G3, G4, J, Ring A, n and R3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.

Scope and limitations of Pd2(dba)3/P(i-BuNCH 2CH2)3N-catalyzed Buchwald-Hartwig amination reactions of aryl chlorides

Proazaphosphatrane ligands in combination with Pd2(dba) 3 generate highly active catalysts for Buchwald-Hartwig amination of aryl chlorides. In particular, commercially available P(i-BuNCH 2-CH2)3N is a highly general and efficient ligand, allowing the coupling of an electronically diverse set of aryl chlorides, including chloropyridines, with a wide variety of amines using 1 mol % of Pd at 100 °C. Either a 1:1 or 2:1 ratio of ligand to Pd was found to be effective. This catalyst system performs exceptionally well for sterically hindered substrates, even with only 0.25 mol % of Pd. It is shown that NaOH can also be used as the base (instead of NaO-t-Bu) allowing functionalized substrates to participate in these reactions.