84175-48-4

Upstream product

• 779-89-5 3-(trifluoromethyl)cinnamic acid 
• 917-54-4 methyllithium 
• 454-89-7 3-Trifluoromethylbenzaldehyde 
• 67-64-1 acetone 
• 2740-83-2 3-(TRIFLUOROMETHYL)BENZYLAMINE 
• 705-28-2 1-ethynyl-3-trifluoromethylbenzene 
• 1439-36-7 1-triphenylphosphoranylidene-2-propanone 
• 1423-26-3 (meta-(trifluoromethyl)phenyl)boronic acid 

Downstream Products

• 84175-35-9 5-(4-morpholinyl)-1-(3-(trifluoromethyl)phenyl)-1-penten-3-one hydrochloride 
• 1173694-13-7 4-(3-(trifluoromethyl)phenyl)butan-2-amine hydrochloride 
• 1228699-91-9 (E)-dimethyl 2-hydroxy-4-(3-(trifluoromethyl)phenyl)but-3-en-2-ylphosphonate 
• 52451-42-0 4-Ethoxy-2-oxo-6-(3-trifluoromethyl-phenyl)-cyclohex-3-enecarboxylic acid ethyl ester 
• 205129-31-3 C₂₀H₁₅F₃O₄ 

Relevant academic research and scientific papers

Piperlongumine derivative as well as preparation method and application thereof

The invention discloses a Piperlongumine derivative as well as a preparation method and application thereof. The Piperlongumine derivative has the following structure: the Piperlongumine derivative provided by the invention contains a plurality of Michael addition receptor units, and the novel structure improves the electrophilicity, so that the Piperlongumine derivative has good protein targetingpotential, and the Piperlongumine derivative has a good inhibition effect on thioredoxin reductase; in an antitumor bioactive in-vitro screening experiment, the derivative also has a certain inhibition effect on the growth of tumor cells, and meanwhile, the derivative has an effect of promoting the generation of active oxygen in A549 human lung cancer cells.

Catalytic Enantioselective Conjugate Addition of Stereodefined Di- and Trisubstituted Alkenylaluminum Compounds to Acyclic Enones

Catalytic enantioselective conjugate addition (ECA) reactions with readily accessible and stereochemically defined E-, Z-, di- and trisubstituted alkenyl aluminum compounds are disclosed. Transformations are promoted by various NHC-copper catalysts (NHC=N-heterocyclic carbene), which are derived from enantiomerically pure sulfonate imidazolinium salts. The desired products were obtained in up to 89% yield and >99:1 e.r.; the alkenyl moiety was transferred with complete retention of its stereochemical identity in all instances. The scope and limitations of the approach, key mechanistic attributes, and representative functionalization are presented as well. (Figure presented.).

Discovery of novel 5-methyl-1H-pyrazole derivatives as potential antiprostate cancer agents: Design, synthesis, molecular modeling, and biological evaluation

Androgen receptor (AR) signaling functions as a core driving force for the progression of prostate cancer (PCa), and AR has been proved to be an effective therapeutic target even for castration-resistant prostate cancer (CRPC). Herein, structural modification via a fragments splicing strategy was performed based on two lead compounds T3 and 10e, leading to the discovery of a series of 5-methyl-1H-pyrazole derivatives. AR reporter gene assay revealed compounds A13 and A14 as potent AR antagonists. Some of the compounds in this series inhibited growth of PCa LNCaP cells more efficiently than enzalutamide. A13 and A14 also showed improved metabolic stability compared with 10e in human liver microsomes.

Rh(III)-Catalyzed Enaminone-Directed Alkenyl C-H Activation for the Synthesis of Salicylaldehydes

A Rh(III)-catalyzed enaminone-directed alkenyl C-H coupling with alkynes for the synthesis of salicylaldehyde derivatives is reported. This represents a unique example of benzene ring framework formation through a transition-metal-catalyzed, directed C-H activation strategy. The two incorporated reactive functionalities, aldehyde and hydroxy groups, provide convenient synthetic handles for further structural elaboration.

Diastereoselective synthesis of β-amino ketone and acid derivatives by palladium-catalyzed conjugate addition

The first diastereoselective synthesis of β-amino ketone and β-amino acid derivatives by palladium-catalyzed conjugate addition of arylboronic acids to chiral β-enamino ketones and β-enamino esters is reported. The catalytic system employing (S)-4-(tert-butyl)oxazolidin-2-one as the chiral auxiliary in water under an air atmosphere provides β-amino ketone and β-amino acid derivatives in high yields with excellent diastereoselectivity.

Design, synthesis and biological evaluation of novel C3-functionalized oxindoles as potential Pim-1 kinase inhibitors

A novel series of C3-functionalized oxindoles, 3-(2-oxo-4-phenylbut-3-en-1-ylidene)indolin-2-ones, were designed, synthesized and investigated for inhibition of cell proliferation against different types of human cancer cell lines, including SW620, HeLa and A549. This biological study showed that these compounds containing the scaffolds of indole and aromatic α,β-unsaturated ketone had moderate to significant antitumor activities. Further study suggested that compound 4b, as one of this kind of structure derivative, showed broad-spectrum antitumor activities against MCF-7, PC-3, SKOV-3, U87, SMMC-7721, SY5Y and A875 cancer cell lines. Besides, the results of the inhibition of Pim kinases indicated that compound 4b showed selective and efficient anti-Pim-1 kinase activity (IC50 = 5 μM). Docking simulation, flow cytometry (FCM), and Hoechst 33342 staining assay suggested that the most active compound 4b induced cell death through apoptosis via binding to the active ATP pocket of Pim-1. Moreover, it showed that compound 4b had strong inhibition of tubulin polymerization which may be caused by inhibiting Pim-1. This journal is

Copper-catalyzed one-pot oxidation-aldol/henry reaction of benzylic amines to α,β-unsaturated methyl ketone/nitro compounds

A novel one-pot synthesis of α,β-unsaturated methyl ketone/nitro compounds from benzylic amines through an oxidation-aldol/Henry reaction is reported. The reaction proceeded well by using MCPBA as oxidant and CuCl 2·2H2O as catalyst. A variety of functionalized α,β-unsaturated methyl ketone/nitro compounds were assembled in moderate yields by application of this catalytic one-pot reaction. Georg Thieme Verlag Stuttgart New York.

Asymmetric crossed-conjugate addition of nitroalkenes to enones by a chiral bifunctional diamine organocatalyst

The crossed-conjugate addition involving the electronwithdrawing group (EWG) of activated alkenes is considered one of the most important C-C bond-forming reactions in organic synthesis. Among them, the β,β-disubstituted nitroolefins as powerful synthons have attracted considerable attention recently because the functionalized products can undergo transformations into useful skeletons. Asymmetric intermolecular crossed-conjugate addition between β-alkyl nitroalkenes and a,b-unsaturated carbonyl compounds to provide allylic nitro compounds with multiple stereogenic centers is still rare. The key challenges are to avoid the homo-crossed addition and realize perfect stereochemical control. Shi and co-workers developed the first asymmetric crossed-conjugate addition of β-alkyl nitroalkenes and enals catalyzed by a chiral diphenylprolinol though a dual activation strategy using a stoichiometric amount of (MeO)3P as a Lewis base (LB) (Scheme 1, path A). Although the secondary amines proved to be effective catalysts in the crossed-Michael addition of nitro activated olefins to carbonyl compounds through the LB nucleophilic mechanism, the enantioselective process awaits further investigation.We envisioned that a chiral diamine catalyst would promote the enantioselective crossed-conjugate addition by a bifunctional activation approach (Scheme 1, path B). Herein, we report the chiral primary-secondary diamine Bronsted acid catalyzed asymmetric crossed-conjugate addition of β-methyl nitroalkenes with α, β-unsaturated acyclic and cyclic ketones with excellent enantioselectivities under mild conditions.

Room temperature aldol reactions using magnetic Fe3O 4@Fe(OH)3 composite microspheres in hydrogen bond catalysis

Fe3O4@Fe(OH)3 composite microspheres are highly active, environmentally friendly and easy to recycle catalysts for aldol reactions, which are catalyzed by a solid-liquid interfacial hydrogen bond catalyst at room temperature.

Unsaturated oxime ethers and their use as fungicides and insecticides

Compounds with fungicidal and insecticidal properties having formula wherein X is N or CH; Y is O, S or NR6; A is independently hydrogen, halo, cyano, (C1-C12)alkyl, or (C1-C12)alkoxy; R1and R6is independently hydrogen or (C1-C4)alkyl; R2is independently hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic(C1-C4)alkyl; R3is independently hydrogen or (C1-C4)alkyl; R4and R5is independently hydrogen, (C1-C4)alkyl, aryl, aralkyl, aryl(C2-C8)alkenyl, aryl(C2-C8)alkynyl, heterocyclic, or heterocyclic(C1-C4)alkyl wherein if one of R4and R5is hydrogen or (C1-C4)alkyl than the other of R4and R5is other than hydrogen or (C1-C4)alkyl, and its enantiomers and stereoisomers and agronomically acceptable salts.