50868-68-3

Usage

Uses

Used in Organic Synthesis:
(2E)-3-(5-Bromo(2-thienyl))prop-2-enoic acid is utilized as a building block in organic synthesis for the creation of a range of pharmaceuticals, agrochemicals, and materials. Its unique structure allows it to be a key component in the development of new compounds with specific properties.
Used in Research:
In the research field, (2E)-3-(5-Bromo(2-thienyl))prop-2-enoic acid serves as an important tool for studying chemical reactions and mechanisms, given its reactivity and the possibility to form various derivatives.
Used in Pharmaceutical Development:
(2E)-3-(5-Bromo(2-thienyl))prop-2-enoic acid is used as a precursor in the development of new drugs and biologically active compounds. Its unique structural features may contribute to the discovery of novel therapeutic agents with improved efficacy and selectivity.
Used in Agrochemical Production:
(2E)-3-(5-Bromo(2-thienyl))prop-2-enoic acid is also employed in the agrochemical industry, where it may be used to develop new pesticides or herbicides, potentially enhancing crop protection and yield.
Used in Material Science:
(2E)-3-(5-Bromo(2-thienyl))prop-2-enoic acid may find applications in material science, where its properties could be leveraged to create new materials with specific characteristics for various industrial uses.
It is important to handle (2E)-3-(5-Bromo(2-thienyl))prop-2-enoic acid with care due to its potential health and environmental risks, which are associated with its chemical properties. Proper safety measures should be taken during its production, use, and disposal to mitigate any adverse effects.

InChI:InChI=1/C7H5BrO2S/c8-6-3-1-5(11-6)2-4-7(9)10/h1-4H,(H,9,10)/b4-2+

Upstream product

• 4701-17-1 5-bromo-2-thiophencarboxaldehyde 
• 141-82-2 malonic acid 
• 151451-43-3 ethyl (E)-3-(5-bromothiophen-2-yl)acrylate 

Downstream Products

• 62157-62-4 3-(5'-bromothiophen-2'-yl)-(E)-propenoic acid methyl ester 
• 28948-60-9 2-bromothieno[3,2-c]pyridin-4(5H)-one 

Relevant academic research and scientific papers

Novel 2-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole and 3-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole derivatives as dengue virus inhibitors targeting NS5 polymerase

Using a functional high-throughput screening (HTS) and subsequent SAR studies, we have discovered a novel series of non-nucleoside dengue viral polymerase inhibitors. We report the elaboration of SAR around hit compound 1 as well as the synthesis and anti

Discovery of Pyrazolo[1,5-a]pyrazin-4-ones as Potent and Brain Penetrant GluN2A-Selective Positive Allosteric Modulators Reducing AMPA Receptor Binding Activity

N-Methyl-D-aspartate receptors (NMDARs) are members of the ionotropic glutamate receptor family and play a crucial role in learning and memory by regulating synaptic plasticity. Activation of NMDARs containing GluN2A, one of the NMDAR subunits, has recent

Synthesis and evaluation of bifunctional PTP4A3 phosphatase inhibitors activating the ER stress pathway

We developed JMS-053, a potent inhibitor of the dual specificity phosphatase PTP4A3 that is potentially suitable for cancer therapy. Due to the emerging role of the unfolded protein response (UPR) in cancer pathology, we sought to identify derivatives that combine PTP4A3 inhibition with induction of endoplasmatic reticulum (ER) stress, with the goal to generate more potent anticancer agents. We have now generated bifunctional analogs that link the JMS-053 pharmacophore to an adamantyl moiety and act in concert with the phosphatase inhibitor to induce ER stress and cell death. The most potent compound in this series, 7a, demonstrated a ca. 5-fold increase in cytotoxicity in a breast cancer cell line and strong activation of UPR and ER stress response genes in spite of a ca. 13-fold decrease in PTP4A3 inhibition. These results demonstrate that the combination of phosphatase inhibition with UPR/ER-stress upregulation potentiates efficacy.

IN-FLOW PHOTOOXYGENATION OF AMINOTHIENOPYRIDINONES GENERATES NOVEL PTP4A3 PHOSPHATASE INHIBITORS

The disclosure provides compounds that inhibit protein tyrosine phosphatase, such as protein tyrosine phosphatase 4A3 (PTP4A3). The disclosure also provides pharmaceutical compositions, uses, and methods of using the compounds, such as in the treatment of cancers. (I), wherein X is O or NH.

In-flow photooxygenation of aminothienopyridinones generates iminopyridinedione PTP4A3 phosphatase inhibitors

A continuous flow photooxygenation of 7-aminothieno[3,2-c]pyridin-4(5H)-ones to produce 7-iminothieno[3,2-c]pyridine-4,6(5H,7H)-diones has been developed, utilizing ambient air as the sole reactant. N-H Imines are formed as the major products, and excellent functional group tolerance and conversion on gram-scale without the need for chromatographic purification allow for facile late-stage diversification of the aminothienopyridinone scaffold. Several analogs exhibit potent in vitro inhibition of the cancer-associated protein tyrosine phosphatase PTP4A3, and the SAR supports an exploratory docking model.

Synthesis of Enantiomerically Pure Ring-Substituted l -Pyridylalanines by Biocatalytic Hydroamination

Current routes to nitrogen-containing heteroarylalanines involve complex multistep synthesis and are often reliant on protection/deprotection steps and wasteful chromatographic purifications. In order to complement existing methodologies, a convenient telescopic strategy was developed for the synthesis of l-pyridylalanine analogues (12 examples) and other l-heteroarylalanines (5 examples) starting from the corresponding aldehydes. A phenylalanine ammonia lyase (PAL) from Anabaena variabilis was used as the biocatalyst to give conversions ranging between 88 and 95%, isolated yields of 32-60%, and perfect enantiopurity (>99% ee) by employing an additional deracemization cascade where necessary.

Heteroarylacrylamides and their use as pharmaceuticals for the stimulation of the expression of endothelial NO synthase

The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endotheli

NEW COMPOUNDS USEFUL FOR THE TREATMENT OF OBESITY, TYPE II DIABETES AND CNS DISORDERS

The present invention relates to compounds of the general formula (I), wherein P is sulfone or sulfonamide; and A, B, W, X, Y and R3 are as defined in the description;to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes, and/or CNS disorders, to achieve reduction of body weight and of body weight gain.

Tetrazole amide derivatives of heterocyclic alkenyl acid and their use as antiallergic substances

Tetrazole amide derivatives of heterocyclic alkenyl acids, of general formula STR1 in which Y=NH, O or S when m=1; Y=N when m=2; m=1 or 2; l=0 or 4; R=H, C1-4 alkyl, Cl, Br, CF3, CH2 OCOCH3, or OCH2 -Ph; R1 =H, alkaline metal or alkaline earth metal, the double bond of the alkenyl chain being of trans or cis configuration and the possible benzene ring being unsubstituted or substituted. Such derivatives possess high antiallergic activity.

Tetrazole amide derivatives of heterocyclic alkenyl acids and their use as antiallergic substances

Tetrazole amide derivatives of heterocyclic alkenyl acids, of general formula (I): in which, Y = NH, O or S when m = 1;, Y = N when m = 2;, m = 1 or 2;, l = 0 or 4;, R = H, C1 4 alkyl, Cl, Br, CF3, CH2OCOCH3, or OCH2-Ph;, R1 = H, alkaline metal or alkaline earth metal;, the double bond of the alkenyl chain being of trans or cis configuration and the possible benzene ring being unsubstituted or substituted. Said derivatives possess high antiallergic activity.