79757-77-0

Usage

Uses

Used in Pharmaceutical Industry:
(4-BROMO-2-THIENYL)METHANOL is used as a building block for the synthesis of various pharmaceuticals. Its unique structure allows for the creation of new compounds with potential therapeutic properties, contributing to the development of innovative medications.
Used in Agrochemical Industry:
(4-BROMO-2-THIENYL)METHANOL is also used as a building block in the synthesis of agrochemicals. Its versatility enables the production of new compounds with applications in agriculture, such as pesticides and herbicides, to improve crop protection and yield.

InChI:InChI=1/C5H5BrOS/c6-4-1-5(2-7)8-3-4/h1,3,7H,2H2

Upstream product

• 18791-75-8 4-Bromothiophen-2-aldehyde 

Downstream Products

• 192441-08-0 6-((4-bromothiophen-2-yl)methoxy)-9H-purin-2-amine 
• 1007388-25-1 ((4-bromothiophen-2-yl)methoxy)(tert-butyl)diphenylsilane 
• 170859-70-8 4-bromo-2-(chloromethyl)thiophene 
• 230623-74-2 (4-{2-[3-(tert-butyl-dimethyl-silanyloxy)-propoxy]-ethyl}-phenyl)-(4-butyl-phenyl)-{4-[2-(4-hexyl-thiophen-2-yl)-vinyl]-phenyl}-amine 
• 230623-75-3 {4-[6-(tert-butyl-dimethyl-silanyloxy)-hexyl]-phenyl}-(4-butyl-phenyl)-{4-[2-(4-hexyl-thiophen-2-yl)-vinyl]-phenyl}-amine 
• 230623-80-0 5-(2-{4-[(4-{2-[3-(tert-butyl-dimethyl-silanyloxy)-propoxy]-ethyl}-phenyl)-(4-butyl-phenyl)-amino]-phenyl}-vinyl)-3-hexyl-thiophene-2-carbaldehyde 
• 230623-76-4 {3-[5-(tert-butyl-dimethyl-silanyloxy)-pentyloxy]-4-[2-(4-hexyl-thiophen-2-yl)-vinyl]-phenyl}-bis-(4-butyl-phenyl)-amine 
• 160005-43-6 2-(4-bromothiophen-2-yl)acetonitrile 
• 1192224-56-8 3-[1-(4-bromothiophen-2-ylmethyl)-6-oxo-1,6-dihydropyridazin-3-yl]benzonitrile 
• 1374690-78-4 C₂₂H₂₀N₂O₃S 
• 1374690-77-3 C₂₂H₂₀N₂O₄S 
• 913828-99-6 {5-[5-(3-chloro-4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-4-ethyl-2-thienyl}methanol 

Relevant academic research and scientific papers

PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT MEDIATED DISORDERS

This disclosure provides pharmaceutical compounds to treat medical disorders, such as complement-mediated disorders, including complement Cl -mediated disorders.

CEPHEM COMPOUNDS, THEIR PRODUCTION AND USE

Cephem compounds, pharmaceutically acceptable salts thereof, and methods of using same, wherein the compound has a bicyclic nitrogen-containing aromatic heterocyclic ring as the quaternary ammoniomethyl group at the 3-position and one or both of a termina

Palladium-catalyzed regioselective allylation of five-membered heteroarenes with allyltributylstannane

Palladium-catalyzed allylation reactions of 2-(chloromethyl)thiophenes, 2-(chloromethyl)furans, and N-protected 2-(chloromethyl)-1H-pyrroles with allyltributylstannane were described in this study. This type of allylation reaction regioselectively occurred on the heteroarene rings to produce allylated dearomatization products or allylated heteroarenes with satisfactory yields.

AMIDINE SUBSTITUTED BETA - LACTAM COMPOUNDS, THEIR PREPARATION AND USE AS ANTIBACTERIAL AGENTS

The present invention relates to novel β-lactam compounds of formula (I), their preparation and use. In particular, this invention relates to novel β-lactam compounds which are amidine substituted monobactam derivatives useful as antimicrobial agents and their preparation.

Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist

S1P3-sparing S1P1 agonists have attracted attention as a suppressant of autoimmunity with reduced side effects. Our synthetic efforts and extensive SAR studies led to the discovery of 10b named CS-2100 with the EC50 value of 4.0 nM for human S1P1 and over 5000-fold selectivity against S1P3. The in vivo immunosuppressive efficacy was evaluated in rats on host versus graft reaction and the ID 50 value was determined at 0.407 mg/kg. The docking studies of CS-2100 with the homology model of S1P1 and S1P3 showed that the ethyl group on the thiophene ring of CS-2100 was sterically hindered by Phe263 in S1P3, not in the case of Leu276 in S1P1. This observation gives an explanation for the excellent S1P3-sparing characteristic of CS-2100.

Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P3-sparing S1P1 agonists

We have previously disclosed 1,2,4-oxadiazole derivative 3 as a potent S1P3-sparing S1P1 agonist. Although compound 3 exhibits potent and manageable immunosuppressive efficacy in various in vivo models, recent studies have revealed that its 1,2,4-oxadiazole ring is subjected to enterobacterial decomposition. As provisions for unpredictable issues, a series of alternative compounds were synthesized on the basis of compound 3. Extensive SAR studies led to the finding of 1,3-thiazole 24c with the EC50 value of 3.4 nM for human S1P1, and over 5800-fold selectivity against S1P3. In rat on host versus graft reaction (HvGR), the ID50 value of 24c was determined at 0.07 mg/kg. The pharmacokinetics in rat and monkey is also reported. Compared to compound 3, 24c showed excellent stability against enterobacteria.

Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: Conformational constraint to favor a bioactive conformation

On the basis of our observation that the biaryl substituent of iminopyrimidinone 7 must be in a pseudoaxial conformation to occupy the contiguous S1-S3 subsites of BACE1, we have designed a novel fused bicyclic iminopyrimidinone scaffold intended to favor this bioactive conformation. Strategic incorporation of a nitrogen atom in the new constrained ring allowed us to develop SAR around the S2′ binding pocket and ultimately resulted in analogues with low nanomolar potency for BACE1. In particular, optimization of the prime side substituent led to major improvements in potency by displacement of two conserved water molecules from a region near S2′. Further optimization of the pharmacokinetic properties of this fused pyrrolidine series, in conjunction with facile access to a rat pharmacodynamic model, led to identification of compound 43, which is an orally active, brain penetrant inhibitor that reduces Aβ40 in the plasma, CSF, and cortex of rats in a dose-dependent manner.

NOVEL HETEROCYCLIC ACRYLAMIDES AND THEIR USE AS PHARMACEUTICALS

The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.

Preparation of 1,4-bis(2-ethynyl-3-thienyl) benzene derivatives linked by oligo(ethyleneglycol) chain

1-(2-Phenylethynyl-3-thienyl)-4-[2-(triisopropylsilyl)ethynyl-3-thienyl] benzene derivative, bearing both a polar oligo(ethyleneglycol) chain and hydrophobic alkyl chains, was prepared. The triisopropylsilyl group was then removed by tetrabutylammonium fl

AMIDO-THIOPHENE COMPOUNDS AND THEIR USE AS 11-BETA-HSD1 INHIBITORS

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc. Formula (I).