13349-90-1

Usage

Uses

Used in Pharmaceutical Industry:
1-(2,2,2-Trifluoroethyl)piperazine is used as a key intermediate in the synthesis of various drugs, leveraging its reactivity in chemical reactions to form new medicinal compounds with potential therapeutic effects.
Used in Agrochemical Industry:
Similarly, in agrochemicals, 1-(2,2,2-Trifluoroethyl)piperazine serves as a building block for the creation of pesticides, contributing to the development of effective crop protection agents.
Used in Organic Chemistry Research:
1-(2,2,2-Trifluoroethyl)piperazine is utilized as a reagent in the preparation of novel organic compounds, exploring its potential to yield new substances with biological activity, thus advancing the discovery of innovative chemical entities.
Used in Coordination Chemistry:
As a ligand, 1-(2,2,2-Trifluoroethyl)piperazine is applied in coordination chemistry to form complexes with metal ions, which can exhibit unique properties and applications in various fields, such as catalysis and materials science.
Used in Catalysis:
1-(2,2,2-Trifluoroethyl)piperazine also serves as a substrate in catalytic reactions, where it participates in processes that can enhance the efficiency and selectivity of chemical transformations, contributing to green chemistry and sustainable processes.

InChI:InChI=1/C6H11F3N2/c7-6(8,9)5-11-3-1-10-2-4-11/h10H,1-5H2

Upstream product

• 13349-91-2 1-(2,2,2-trifluoroethyl)piperazine hydrochloride 
• 77278-37-6 4-(2,2,2-trifluoroacetyl)piperazine-1-carboxylic acid tert-butyl ester 
• 692058-21-2 4-(2,2,2-trifluoroethyl)piperazin-1-carboxylic acid tert-butyl ester 
• 629625-96-3 benzyl 4-(2,2,2-trifluoroethyl)piperazine-1-carboxylate 

Downstream Products

• 1404536-38-4 C₃₂H₃₅F₃N₆O₃ 
• 1353628-75-7 C₂₅H₂₈Cl₂F₃N₇O₃S 
• 1296374-20-3 N-methyl-3-nitro-4-[4-(2,2,2-trifluoroethyl)-1-piperazinyl]benzenesulfonamide 
• 252672-44-9 2-[2-Ethoxy-5-(4-(2,2,2-trifluoroethyl)-piperazine-1-sulphonyl)-phenyl]-7-(1-ethylpropyl)-5-methyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one 

Relevant academic research and scientific papers

Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and in Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model

A series of 2,4-disubstituted imidazopyridines, originating from a SoftFocus Kinase library, was identified from a high throughput phenotypic screen against the human malaria parasite Plasmodium falciparum. Hit compounds showed moderate asexual blood stage activity. During lead optimization, several issues were flagged such as cross-resistance against the multidrug-resistant K1 strain, in vitro cytotoxicity, and cardiotoxicity and were addressed through structure-Activity and structure-property relationship studies. Pharmacokinetic properties were assessed in mice for compounds showing desirable in vitro activity, a selectivity window over cytotoxicity, and microsomal metabolic stability. Frontrunner compound 37 showed good exposure in mice combined with good in vitro activity against the malaria parasite, which translated into in vivo efficacy in the P. falciparum NOD-scid IL-2Rnull (NSG) mouse model. Preliminary mechanistic studies suggest inhibition of hemozoin formation as a contributing mode of action.

Cyclin-dependent kinase inhibitors and application thereof

The invention relates to compounds used as cyclin-dependent kinase inhibitors and application thereof, belonging to the field of medical chemistry. Specifically, the invention provides the compound asshown in a formula I which is described in the specification, or isomers, pharmaceutically acceptable salts, solvates, crystals or prodrugs thereof, preparation methods thereof, pharmaceutical compositions containing the compounds, and application of the compounds or the compositions to treatment of cancer, tissue hyperplasia diseases or inflammatory diseases. The compounds of the invention havegood inhibitory activity to CDK7 and are highly expected to be developed into a therapeutic agent for cancer, tissue hyperplasia diseases and inflammatory diseases.

BIS-HETEROARYL DERIVATIVES AS MODULATORS OF PROTEIN AGGREGATION

The present invention relates to certain bis-heteroaryl compounds, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto- temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer including melanoma.

Aryl alkynyl hydrocarbon compound and preparation method and application thereof

The invention relates to an aryl alkynyl hydrocarbon compound and a medicine compound containing the compound. The compound or the medicine compound can serve as an inhibitor of Retinoid-related orphan receptor gamma t (RORyt). The invention further relates to a method for preparing the compound and the medicine compound and application thereof to mammal treatment or prevention, especially RORyt mediated inflammation of humans or autoimmune diseases.

NOVEL COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME

The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, isomers thereof, or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions comprising the same, a method of treating disease using the composition, and methods for preparing the novel compounds. The novel compounds according to the present invention have histone deacetylase 6 (HDAC6) inhibitory activity, and are effective for the prevention or treatment of HDAC6-associated diseases, including cancer, inflammatory diseases, autoimmune diseases, neurological diseases and neurodegenerative disorders.

Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties

Based on the previously reported clinical candidate, AMG 517 (compound 1), a series of related piperazinylpyrimidine analogues were synthesized and evaluated as antagonists of the vanilloid 1 receptor (VR1 or TRPV1). Optimization of in vitro potency and physicochemical and pharmacokinetic properties led to the discovery of (R)-N-(4-(6-(4-(1-(4-fluorophenyl)ethyl) piperazin-1-yl)pyrimidin-4-yloxy)benzo[d]-thiazol-2-yl)acetamide (16p), a potent TRPV1 antagonist [rTRPV1(CAP) IC50 = 3.7 nM] with excellent aqueous solubility (≥200 μg/mL in 0.01 N HCl) and a reduced half-life (rat t 1/2 = 3.8 h, dog t1/2 = 2.7 h, monkey t1/2 = 3.2 h) as compared to AMG 517. In addition, compound 16p was shown to be efficacious at blocking a TRPV1-mediated physiological response in vivo (ED 50 = 1.9 mg/kg, p.o. in the capsaicin-induced flinch model in rats) and was also effective at reducing thermal hyperalgesia induced by complete Freund's adjuvant in rats (MED = 1 mg/kg, p.o). Based on its improved overall profile, compound 16p (AMG 628) was selected as a second-generation candidate for further evaluation in human clinical trials as a potential new treatment for chronic pain.

NOVEL PHYSIOLGICALLY ACTIVE SUBSTANCES

The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.

QUINAZOLINE DERIVATIVES AS SRC TYROSINE KINASE INHIBITORS

The invention concerns quinazoline derivatives of Formula (I): (A chemical formula should be inserted here - please see paper copy enclosed herewith) wherein Z is an O, S, SO, SO2, N(R2) or C(R2)2 group wherein each R2 group is hydrogen or (1-8C) alkyl, m is 0, 1, 2 or 3, each R1 group is selected from halogeno, (1-8C) alkyl, (1-6C) alkoxy and any of the other meanings defined in the description, n is 0, 1, 2 or 3, and each R3 group is selected from halogeno, (1-8C) alkyl, (1-6C) alkoxy and any of the other meanings defined in the description, or pharmaceutically-acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.