509073-62-5

Usage

Uses

Used in Pharmaceutical Industry:
TERT-BUTYL 4-(4-NITROBENZOYL)TETRAHYDRO-1(2H)-PYRAZINECARBOXYLATE is used as a building block for the synthesis of pharmaceutical compounds due to its unique structure and properties. Its potential biological or pharmaceutical applications are currently being explored, which may lead to the development of new drugs and therapies.
Used in Organic Synthesis:
In the field of organic synthesis, TERT-BUTYL 4-(4-NITROBENZOYL)TETRAHYDRO-1(2H)-PYRAZINECARBOXYLATE serves as a key intermediate for the creation of various organic compounds. Its versatility in chemical reactions allows for the synthesis of a wide range of products, contributing to the advancement of organic chemistry.

Upstream product

• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 62-23-7 4-nitro-benzoic acid 
• 122-04-3 4-nitro-benzoyl chloride 

Downstream Products

• 350684-49-0 4-(4-aminobenzoyl)piperazine-1-carboxylic acid tert-butyl ester 
• 72141-41-4 (4-nitro-phenyl)-piperazin-1-yl-methanone 
• 1622867-09-7 C₂₅H₂₁N₅O₅S 

Relevant academic research and scientific papers

Synthesis of novel sulfonamide derivatives containing pyridin-3-ylmethyl 4-(benzoyl)piperazine-1-carbodithioate moiety as potent PKM2 activators

Pyruvate kinase M2 isoform (PKM2) plays a key role in cancer progression through both metabolic and non-metabolic functions, thus it is recognized as a potential target for cancer diagnosis and treatment. In this study, we discovered a sulfonamide-dithiocarbamate compound 8a as a novel PKM2 activator from a random screening of an in-house compound library. Then, a series of lead compound 8a analogs were designed and synthesized for screening as potent PKM2 activators. Among them, compound 8b (AC50 = 0.136 μM) and 8k (AC50 = 0.056 μM) showed higher PKM2 activation activities than positive control NZT (AC50 = 0.228 μM), and they (IC50 50 > 10 μM). Especially, compound 8k inhibited the proliferation of multiple cancer cells, but showed little toxicity on normal cells. In addition, we found that compound 8k inhibit the colony formation of MCF7 cells. Western blot analysis demonstrated that 8k could reduce PKM2 nuclear localization and block the downstream signaling pathway of PKM2, resulting in suppression of tumor cell proliferation. Overall, compound 8k may be a promising candidate for further mechanistic investigation of PKM2 and cancer therapy.

Memantine urea derivative as well as preparation method and application thereof

The invention provides a memantine urea derivative as well as a preparation method and application thereof, and relates to the technical field of medicines. The memantine urea derivative provided by the invention has a typical urea structure as a primary

Optimization and SAR research at the piperazine and phenyl rings of JNJ4796 as new anti-influenza A virus agents, part 1

JNJ4796, a small molecule fuse inhibitor targeting the conserved stem region of hemagglutinin, effectively neutralized a broad spectrum of group 1 influenza A virus (IAV), and protected mice against lethal and sublethal influenza challenge after oral admi

Pyridine compound, preparation method and application thereof, and pharmaceutical composition

The invention provides a pyridine compound as well as a preparation method and application thereof, and belongs to the technical field of medical chemistry. The pyridine compound provided by the invention has excellent in-vitro antiviral activity and potential druggability, and is expected to become a clinical candidate molecule for overcoming influenza.

Aminodithioformate compound used as FAK inhibitor

A purpose of the invention is to provide an aminodithioformate compound serving as an FAK inhibitor, a pharmaceutical composition, a preparation method and applications thereof, wherein the compound has a structure represented by the following general formula (I).

Looking toward the Rim of the Active Site Cavity of Druggable Human Carbonic Anhydrase Isoforms

We report the synthesis and biochemical evaluation of a series of substituted 4-(4-aroylpiperazine-1-carbonyl)benzenesulfonamides (5a-s) developed as inhibitors of druggable carbonic anhydrase (CA) isoforms, as tools for the identification of new therapeu

SMALL MOLECULE PROTEOLYSIS-TARGETING CHIMERAS AND METHODS OF USE THEREOF

Novel small molecule proteolysis-targeting chimeras (PROTACs) are provided, along with methods for their use as Bruton's tyrosine kinase (BTK) degraders. The small molecule PROTACs described herein are useful in treating and/or preventing BTK-related diseases, such as cancer, neurodegenerative disorders, inflammatory diseases, and metabolic disorders. Also provided are methods for inducing BTK degradation in a cell using the compounds and compositions described herein. Exemplary compounds include: (I).

Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities

A series of 2,4-diarylaminopyrimidine derivatives containing dithiocarbamate moiety were designed by molecular hybridization strategy and synthesized for screening as inhibitors of focal adhesion kinase (FAK). Most of these compounds exhibit significant a

DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE

The present application provides bifunctional compounds of Formula X or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.

Substituted O-hydroxyphenyl ketone compound as well as preparation method and application thereof

The invention discloses a substituted O-hydroxyphenyl ketone compound, a preparation method of the substituted O-hydroxyphenyl ketone compound, and an application of the substituted O-hydroxyphenyl ketone compound to preparation of a BRD4 protein activity