234082-33-8

Usage

Uses

Used in Medicinal Chemistry:
Tert-butyl 4-(4-(ethoxycarbonyl)phenyl)piperazine-1-carboxylate is used as a synthetic intermediate for the development of various bioactive molecules. Its unique structural features allow for the creation of compounds with specific biological activities, making it a valuable asset in the design and synthesis of novel therapeutic agents.
Used in Pharmaceutical Research:
In the pharmaceutical industry, tert-butyl 4-(4-(ethoxycarbonyl)phenyl)piperazine-1-carboxylate is employed as a key component in the synthesis of drug candidates. Its versatility in chemical reactions enables the production of a wide range of molecules with potential therapeutic applications, particularly in the treatment of central nervous system disorders.
Used in Drug Discovery:
As a piperazine derivative, tert-butyl 4-(4-(ethoxycarbonyl)phenyl)piperazine-1-carboxylate may exhibit affinity for specific receptor targets and biological pathways. This property makes it an attractive candidate for drug discovery efforts, where it can be further optimized to enhance its pharmacological properties and selectivity for desired targets.
Used in Central Nervous System Disorders Treatment:
Tert-butyl 4-(4-(ethoxycarbonyl)phenyl)piperazine-1-carboxylate has been studied for its potential therapeutic effects in the context of central nervous system disorders. Its ability to modulate specific biological pathways and interact with receptor targets makes it a promising candidate for the development of treatments for various neurological conditions.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 80518-57-6 ethyl 4-(piperazin-1-yl)benzoate 
• 451-46-7 4-fluorobenzoic acid ethyl ester 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 123-91-1 1,4-dioxane 
• 5798-75-4 Ethyl 4-bromobenzoate 
• 17159-79-4 ethyl 4-oxocyclohexane-1-carboxylate 

Downstream Products

• 162046-66-4 4-(4-(1,1-dimethylethoxycarbonyl)piperazin-1-yl)benzoic acid 
• 406233-75-8 3-nitro-4-((2-(phenylthio)ethyl)amino)-N-(4-piperazin-1-ylbenzoyl)benzenesulfonamide 
• 406231-38-7 4-{4-[3-nitro-4-(2-phenylsulfanyl-ethylamino)-benzenesulfonylaminocarbonyl]-phenyl}-piperazine-1-carboxylic acid tert-butyl ester 
• 163210-45-5 4-[4-(2-benzenesulfonylamino-2-tert-butoxycarbonyl-ethylcarbamoyl)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 163209-37-8 (S)-2-Benzenesulfonylamino-3-(4-piperazin-1-yl-benzoylamino)-propionic acid 
• 80518-57-6 ethyl 4-(piperazin-1-yl)benzoate 
• 1374882-66-2 {(S)-1-[(S)-2-(4-{4'-[4-(4-cyclopropanecarbonyl-piperazin-1-yl)-benzoylamino]-biphenyl-4-yl}-1H-imidazol-2-yl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid methyl ester 
• 1018631-34-9 4-(4-cyclopropanecarbonyl-piperazin-1-yl)-benzoic acid 
• 1374891-49-2 N-(4-bromo-phenyl)-4-(4-cyclopropanecarbonyl-piperazin-1-yl)-benzamide 
• 1374891-52-7 (S)-2-(4-{4'-[4-(4-Cyclopropanecarbonyl-piperazin-1-yl)-benzoylamino]-biphenyl-4-yl}-1H-imidazol-2-yl)-pyrrolidine-1-carboxylic acid tert-butyl ester 
• 1374882-70-8 4-[4-(4'-{2-[(S)-1-((S)-2-Methoxycarbonylamino-3-methyl-butyryl)-pyrrolidin-2-yl]-1H-imidazol-4-yl}-biphenyl-4-ylcarbamoyl)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 85474-75-5 4-(piperazin-1-yl)benzoic acid 

Relevant academic research and scientific papers

Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents

To discover antifungal compounds with broad-spectrum and stable metabolism, a series of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives was designed and synthesized. Compounds A30-A34 exhibited excellent broad-spectrum antifungal activity against Candida albicans with MIC values in the range of 0.03–0.5 μg/mL, and against Cryptococcus neoformans and Aspergillus fumigatus with MIC values in the range of 0.25–2 μg/mL. In addition, compounds A31 and A33 showed high metabolic stability in human liver microsomes in vitro, with the half-life of 80.5 min and 69.4 min, respectively. Moreover, compounds A31 and A33 showed weak or almost no inhibitory effect on the CYP3A4 and CYP2D6. The pharmacokinetic evaluation in SD rats showed that compound A31 had suitable pharmacokinetic properties and was worthy of further study.

Electrochemical Cross-Dehydrogenative Aromatization Protocol for the Synthesis of Aromatic Amines

The introduction of amines onto aromatics without metal catalysts and chemical oxidants is synthetically challenging. Herein, we report the first example of an electrochemical cross-dehydrogenative aromatization (ECDA) reaction of saturated cyclohexanones and amines to construct anilines without additional metal catalysts and chemical oxidants. This reaction exhibits a broad scope of cyclohexanones including heterocyclic ketones, affording a variety of aromatic amines with various functionalities, and shows great potential in the synthesis of biologically active compounds.

Protein degradation targeting chimera for degrading androgen receptor

The invention relates to a novel difunctional molecule compound based on VHL ligand induction and application of the difunctional molecule compound in synthesis of the compounds and pharmaceutical compositions thereof. The compound is shown as a formula I. The compound can selectively induce AR protein degradation and can be used for treating cancers such as prostatic cancer and breast cancer.

Benzothiazole compounds and medical application

The invention discloses a benzothiazole compound and medical application thereof, particularly relates to a benzothiazole compound shown as a formula I and medical application thereof, and especiallyrelates to application of the benzothiazole compound serving as a USP7C-terminal structural domain regulating agent in medicines for preventing and treating myelodysplastic syndromes and malignant tumors. The benzothiazole compound shown in the formula I or the pharmaceutically acceptable salt or solvate of the benzothiazole compound has strong binding force with USP7C-terminal protein; and the protein level of DNMT1 in tumor cells can be reduced, so that the compound can be applied to the preparation of USP7 regulators, has a remarkable anti-tumor cell proliferation effect, and can be used for preparing medicines for preventing or treating myelodysplastic syndrome and malignant tumors.

Design and characterization of cereblon-mediated androgen receptor proteolysis-targeting chimeras

Proteolysis-targeting chimera (PROTAC)-mediated protein degradation is a rapidly emerging therapeutic intervention that induces the degradation of targeted proteins. Herein, we report the design and biological evaluation of a series of androgen receptor (AR) PROTAC degraders for the treatment of metastatic castration-resistant prostate cancer. Predominantly, instead of thalidomide, we utilized the TD-106 scaffold, a novel cereblon (CRBN) binder that was identified in our previous study. Our results suggest that the linker position in the TD-106 CRBN binder is critical for the efficiency of AR degradation. The compounds attached to the 6-position of TD-106 promoted better degradation of AR than those at the 5- and 7-positions. Among the synthesized AR PROTACs, the representative degrader 33c (TD-802) effectively induced AR protein degradation, with a degradation concentration 50% of 12.5 nM and a maximum degradation of 93% in LNCaP prostate cancer cells. Additionally, most AR PROTAC degraders, including TD-802, displayed good liver microsomal stability and in vivo pharmacokinetic properties. Finally, we showed that TD-802 effectively inhibited tumor growth in an in vivo xenograft study.

Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors

Fibroblast growth factor receptors (FGFRs) are important targets for cancer therapy. Herein, we describe the design, synthesis, and biological evaluation of a novel series of 1H-pyrazolo[3,4-b]pyridine derivatives as potent and selective FGFR kinase inhibitors. On the basis of its excellent in vitro potency and favorable pharmacokinetic properties, compound 7n was selected for in vivo evaluation and showed significant antitumor activity in a FGFR1-driven H1581 xenograft model. These results indicated that 7n would be a promising candidate for further drug development.

Pyrazolo [3,4 - the b] pyridine and [...] composition preparation method and use of (by machine translation)

The present invention provides a pyrazolo [3,4 - the b] pyridine and [...] compound of preparation and use, in particular, the present invention provides a following formula (I) compounds are shown, wherein the definition of each group as described in the specification. The compounds of the invention has excellent tyrosine kinase inhibiting activity, so can be used for preparing a series of treating diseases associated with the tyrosine kinase activity of the drug. (by machine translation)

INDUCTION OF GATA2 BY HDAC1 AND HDAC2 INHIBITORS

Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with Gata2 deficiency, particularly diseases or disorders that involve any type of HDAC1 and/or HDAC2 expression. Such diseases include acute myeloid leukemia (AML); familial myelodysplastic syndrome (MDS); leukemia; sickle-cell anemia; beta-thalassemia; monocytopenia and mycobacterial infections; dendritic cell, nonocyte, B, and natural killer lymphoid deficiency; Emberger syndrome; asymptomatic neurocognitive impairment; mild neurocognitive disorder; and HIV- associated dementia.

NOVEL INHIBITORS OF HEPATITIS C VIRUS

The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.

APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES

Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.