77279-24-4

Usage

Uses

Used in Pharmaceutical Industry:
TERT-BUTYL 4-(2-HYDROXYETHYL)PIPERAZINE-1-CARBOXYLATE is used as an intermediate in the synthesis of pharmaceuticals for its potential pharmacological properties and as a building block for the development of new drugs.
Used in Agrochemical Industry:
TERT-BUTYL 4-(2-HYDROXYETHYL)PIPERAZINE-1-CARBOXYLATE is used as an intermediate in the synthesis of agrochemicals, contributing to the development of new compounds with biological activities for agricultural applications.

InChI:InChI=1/C11H22N2O3/c1-11(2,3)16-10(15)13-6-4-12(5-7-13)8-9-14/h14H,4-9H2,1-3H3

Upstream product

• 103-76-4 1-(2-hydroxyethyl)piperazine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 540-51-2 2-bromoethanol 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 209667-59-4 tert-butyl 4-(2-ethoxy-2-oxoethyl)piperazine-1-carboxylic acid 
• 34619-03-9 tert-butyldicarbonate 
• 1426682-55-4 t-butyl 4-pyridyl carbonate 
• 89985-91-1 tert-butyl pyridin-2-yl carbonate 
• 245435-42-1 4-(2-formyloxy-ethyl)-piperazine-1-carboxylic acid tert-butyl ester 

Downstream Products

• 658053-32-8 N-[3-(4-hydroxyphenyl)propionyl]-L-isoleucyl-L-proline 2-[4-(tert-butyloxycarbonyl)piperazin-1-yl]ethyl ester 
• 889107-87-3 methyl 2-[2-(4-tert-butoxycarbonylpiperazin-1-yl)ethoxy]-4-methoxybenzoate 
• 1233237-24-5 tert-butyl-4-(2-(4-(5-(2,4-difluorophenoxy)-2-oxo-1,3,4-oxadiazol-3(2H)-yl)phenoxy)ethyl)piperazine-1-carboxylate 
• 1240300-01-9 tert-butyl 4-[2-[4-(1-(benzyloxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)phenoxy]ethyl]piperazine-1-carboxylate 
• 1420290-97-6 4-{2-[4-chloro-2-(2-chloro-4-nitro-phenylcarbamoyl)-phenoxy]-ethyl}-piperazine-1-carboxylic acid tert-butyl ester 
• 1420290-86-3 5-chloro-N-(2-chloro-4-nitro-phenyl)-2-(2-piperazin-1-yl-ethoxy)benzamide 
• 1240299-34-6 6-(4-{4-[2-(4-acetylpiperazin-1-yl)ethoxy]phenyl}piperidin-1-yl)-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine napadisylate 

Relevant academic research and scientific papers

Design, synthesis and antifungal evaluation of borrelidin derivatives

Borrelidin, a nitrile containing 18-membered polyketide macrolide, display potent antifungal activity. In this study, a library of borrelidin derivatives were synthesized. Their structures were elucidated by detailed spectroscopic data analysis. The antifungal activity and cytotoxicity of these target compounds were evaluated by broth microdilution and 3-(4,5-dimethylthiazol-2-yl)-3,5-phenytetrazoliumromide (MTT) methods. Among forty-seven prepared analogues, compound 3b had the inhibitory effect on Candida albicans and Candida parapsilosis (MIC: 50 and 12.5 μg/mL, respectively). Furthermore, compounds 4n and 4r presented better antifungal activity against Aspergillus fumigatus with 12.5 μg/mL MIC value, which were insensitive to borrelidin. Preliminary structure-activity relationships (SAR) revealed that the ester analogues containing fragment -OCH2CH2N- had an important effect on the antifungal activity. Meanwhile, the molecular docking study indicated the carboxyl substituents in BN could provide extra interaction with pathogenic fungal threonyl-tRNA synthetase (ThrRS).

Synthesis and antifungal photodynamic activities of a series of novel zinc(II) phthalocyanines substituted with piperazinyl moieties

A series of novel zinc(II) phthalocyanines tetra-substituted or mono-substituted with piperazinyl moieties linked by different ethoxy chains has been prepared and characterized. The effects of the N-protecting group of piperazinyl moiety, length of ethoxy chains and number of substitutes on the photophysical, photochemical properties, cellular uptakes and in vitro photodynamic antifungal activities have also been examined. All of these compounds are essentially non-aggregated and good singlet oxygen generators with quantum yields (ΦΔ) of 0.54-0.77 in N,N-dimethylformamide. The photodynamic activity of these compounds against Candida albicans follows the order: 7 > 5a > 5b > 4a ≈ 4b. The mono-substituted phthalocyanine 7 exhibits the highest photodynamic inactivation of C. albicans with an IC90 value of 9 μM, which can be attributed to its better amphiphilicity and even higher cellular uptake. The results suggest that phthalocyanine 7 is a potential photosensitizer for antifungal photodynamic therapy.

FUSED PYRIMIDINE PYRIDINONE COMPOUNDS AS JAK INHIBITORS

The disclosure provides compounds of formula (I), or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The disclosure also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat gastrointestinal inflammatory diseases.

METHODS FOR DELAYING, PREVENTING, AND TREATING ACQUIRED RESISTANCE TO RAS INHIBITORS

The present disclosure relates to compositions and methods for the treatment of diseases or disorders (e.g., cancer) with bi-steric inhibitors of mTOR in combination with RAS inhibitors. Specifically, in some embodiments this disclosure includes compositions and methods for inducing apoptosis of tumor cells and/or for delaying, preventing, or treating acquired resistance to RAS inhibitors using bi-steric mTOR inhibitors.

TRICYCLIC COMPOUNDS ACTING ON CRBN PROTEINS

The present invention discloses a series of tricyclic compounds and use thereof in preparing a medicament for treating a disease related to CRBN protein. Specifically, the present invention discloses a derivative compound of formula (1) or a pharmaceutically acceptable salt thereof.

Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against Plasmodium falciparum in Vitro

In the context of drug repositioning and expanding the existing structure-activity relationship around astemizole (AST), a new series of analogues were designed, synthesized, and evaluated for their antiplasmodium activity. Among 46 analogues tested, compounds 21, 30, and 33 displayed high activities against asexual blood stage parasites (PfNF54 IC50 = 0.025-0.043 μM), whereas amide compound 46 additionally showed activity against late-stage gametocytes (stage IV/V; PfLG IC50 = 0.6 ± 0.1 μM) and 860-fold higher selectivity over hERG (46, SI = 43) compared to AST. Several analogues displaying high solubility (Sol > 100 μM) and low cytoxicity in the Chinese hamster ovary (SI > 148) cell line have also been identified.

TAU-PROTEIN TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE

The present disclosure relates to bifunctional compounds, which find utility as modulators of tan protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tan protein, such that tan protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tan. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tan protein. Diseases or disorders that result from aggregation or accumulation of tan protein are treated or prevented with compounds and compositions of the present disclosure.

WEE1 inhibitors as well as preparation and application thereof

The invention relates to WEE1 inhibitors as well as preparation and application thereof. The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, solvates, polymorphs or isomers thereof, and their use in the preparation of medicaments for the treatment of diseases associated with WEE1 activity.

TARGETING DNA REPAIR IN TUMOR CELLS VIA INHIBITION OF ERCC1-XPF

The current application relates to pyronaridine or 6-chloro-2-methoxyacridine analogs having binding affinity for the ERCC1-XPF hetero-dimerization interface. The compounds can be used for targeting DNA repair in tumor cells via ERCC1-XPF inhibition, ther

ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-I' PATHWAY AND METHODS OF USE THEREOF

The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.