75815-46-2

Usage

Uses

Used in Pharmaceutical Industry:
2-BROMO-1-(2-THIENYL)-1-PROPANONE serves as a crucial intermediate in the synthesis of pharmaceuticals, contributing to the development of new drugs and medicinal compounds. Its reactivity facilitates the creation of a diverse array of molecular structures, which can be optimized for specific therapeutic effects.
Used in Agrochemical Industry:
In the agrochemical sector, 2-BROMO-1-(2-THIENYL)-1-PROPANONE is utilized as an intermediate for the production of various agrochemicals. Its role in chemical synthesis allows for the development of compounds that can be used in pest control, crop protection, and other agricultural applications.
Used as a Reagent in Organic Synthesis:
2-BROMO-1-(2-THIENYL)-1-PROPANONE is also employed as a reagent in organic synthesis, where its ability to engage in multiple types of chemical reactions is leveraged to form complex organic molecules. This makes it a valuable tool in the synthesis of fine chemicals and other specialty compounds.
Used in the Manufacture of Fine Chemicals:
As a precursor in the production of fine chemicals, 2-BROMO-1-(2-THIENYL)-1-PROPANONE plays a significant role in the creation of high-purity chemical products used in various industries, including research, cosmetics, and the food industry.

InChI:InChI=1/C7H7BrOS/c1-5(8)7(9)6-3-2-4-10-6/h2-5H,1H3

Upstream product

• 13679-75-9 1-thiophen-2-yl-propan-1-one 

Downstream Products

• 131727-68-9 N-[4-Methoxymethyl-1-(1-methyl-2-oxo-2-thiophen-2-yl-ethyl)-piperidin-4-yl]-N-phenyl-propionamide 
• 81590-68-3 5-chloro-1-[1-(2-thenoyl)ethyl]pyrimidin-2-one 
• 1126519-27-4 (S)-2-phenyl-1-(thiophen-2-yl)propan-1-one 
• 1126518-86-2 (R)-2-phenyl-1-(thiophen-2-yl)propan-1-one 
• 1198567-68-8 6-[3-(tert-butyldimethylsilanyloxymethyl)-2,4-difluorophenyl]-3-methyl-2-thien-2-ylimidazo[1,2-a]pyridine 
• 4506-74-5 2-morpholino-1-(thiophen-2-yl)propan-1-one 
• 1002756-63-9 3-chloro-6-methyl-5-thiophen-2-yl-4-(2,4,6-trifluoro-phenyl)-pyridazine 

Relevant academic research and scientific papers

Enantioconvergent Cu-Catalyzed Radical C-N Coupling of Racemic Secondary Alkyl Halides to Access α-Chiral Primary Amines

α-Chiral alkyl primary amines are virtually universal synthetic precursors for all other α-chiral N-containing compounds ubiquitous in biological, pharmaceutical, and material sciences. The enantioselective amination of common alkyl halides with ammonia is appealing for potential rapid access to α-chiral primary amines, but has hitherto remained rare due to the multifaceted difficulties in using ammonia and the underdeveloped C(sp3)-N coupling. Here we demonstrate sulfoximines as excellent ammonia surrogates for enantioconvergent radical C-N coupling with diverse racemic secondary alkyl halides (>60 examples) by copper catalysis under mild thermal conditions. The reaction efficiently provides highly enantioenrichedN-alkyl sulfoximines (up to 99% yield and >99% ee) featuring secondary benzyl, propargyl, α-carbonyl alkyl, and α-cyano alkyl stereocenters. In addition, we have converted the masked α-chiral primary amines thus obtained to various synthetic building blocks, ligands, and drugs possessing α-chiral N-functionalities, such as carbamate, carboxylamide, secondary and tertiary amine, and oxazoline, with commonly seen α-substitution patterns. These results shine light on the potential of enantioconvergent radical cross-coupling as a general chiral carbon-heteroatom formation strategy.

Enantioselective and Diastereoselective Construction of Chiral Amino Alcohols by Iridium-f-Amphox-Catalyzed Asymmetric Hydrogenation via Dynamic Kinetic Resolution

The iridium-f-amphox-catalyzed asymmetric hydrogenation of racemic α-amino β-unfunctionalized ketones proceeds via a DKR (dynamic kinetic resolution) process for the construction of various chiral N,N-disubstituted α-amino β-unfunctionalized alcohols in quantitative yields with excellent enantioselectivities and diastereoselectivities (all products >99% ee and >99:1 dr, TON up to 100 000). Importantly, this catalytic asymmetric hydrogenation with a DKR process provided a highly efficient and powerful synthetic strategy for the preparation of key chiral intermediates of the preclinical antitumor agent (S,S)-R116010.

CERAMIDE GALACTOSYLTRANSFERASE INHIBITORS FOR THE TREATMENT OF DISEASE

Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme ceramide galactosyltransferase (CGT), such as, for example, lysosomal storage diseases. Examples of lysosomal storage diseases include, for example, Krabbe disease and Metachromatic Leukodystrophy.

Novel preparation of tiaprofenic acid

A new synthesis of the nonsteroidal anti-inflammatory drug tiaprofenic acid starting from thiophene is described. The sequence involves five steps, and the acylation with benzoyl chloride was catalysed by zinc oxide under solventfree conditions at room temperature. This method uses a much cheaper starting material and has a higher total yield (78.4%) than other methods. It is suitable for industrial production.

PYRAZOL-3-ONES THAT ACTIVATE PRO-APOPTOTIC BAX

This application features pyrazol-3-one compounds that activate pro-apoptotic BAX. Also featured are methods of using such compounds, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., insufficient apoptosis of diseased or damaged cells or essentially the absence of apoptosis of diseased or damaged cells).

Catalytic asymmetric cross-couplings of racemic α-bromoketones with arylzinc reagents

(Chemical Equation Presented) Nickel box: The first catalytic asymmetric method for cross-coupling arylzinc reagents with α-bromoketones has been developed (see scheme). This stereoconvergent carbon-carbon bond-forming process occurs under unusually mild conditions and without activators, thereby allowing the generation of potentially labile tertiary stereocenters.

Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction

A series of bupropion (1a) analogues (1b-1ff) were synthesized, and their in vitro and in vivo pharmacological properties evaluated with the goal of developing a 1a analogue that had better properties for treating addictions. Their in vitro pharmacological properties were examined by [3H] dopamine ([3H]DA), [3H]serotonin ([3H]5HT), and [3H]norepinephrine ([3H]NE) uptake inhibition studies, and by binding studies at the dopamine, serotonin, and norepinephrine transporters using [125I]RTI-55 in cloned transporters. Several analogues showed increased [3H]DAuptake inhibition with reduced or little change in [3H]5HT and [3H]NE uptake inhibition relative to bupropion. Thirty-five analogues were evaluated in a 1 h locomotor activity observation test and 32 in an 8 h locomotor activity observation test and compared to the locomotor activity of cocaine. Twenty-four analogues were evaluated for generalization to cocaine drug discrimination after i.p. administration, and twelve analogues were tested in a time course cocaine discrimination study using oral administration. 2-(N-Cyclopropylamino)-3- chloropropiophenone (1x) had the most favorable in vitro efficacy and in vivo pharmacological profile for an indirect dopamine agonist pharmacotherapy for treating cocaine, methamphetamine, nicotine, and other drugs of abuse addiction. 2009 American Chemical Society.

NOVEL PYRIDAZINE DERIVATIVES

The present invention relates to novel pyridazine derivatives of formula I as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is hydrogen, C1-C6alkyl, C1-Csub

Pyrrole derivatives and medicinal composition

The invention relates to a pharmaceutical composition comprising a pyrrole derivative of the following formula [1] or a pharmaceutically acceptable salt thereof, or a solvate of either of them, as an active ingredient. STR1 (wherein R1 represents hydrogen or alkoxycar91 bonylamino, R2 represents alkyl, aryl which may be substituted, aromatic heterocyclyl which may be substituted, unsubstituted amino, monoalkylamino, dialkylamino, or cyclic amino which may be substituted; R3 represents cyano or carbamoyl; R4 represents hydrogen or alkyl; E represents alkylene; q is equal to 0 or 1, A represents methyl, aryl which may be substituted, or aromatic heterocyclyl which may be substituted). The pharmaceutical composition of the invention is effective for the treatment of pollakiuria or urinary incontinence.

Process for preparing α-hydroxy-acids and compounds obtained by this process

The invention relates to a process for preparing α-hydroxy-acids of general formula: STR1 in which R represents hydrogen or a lower alkyl radical and Cy represents a phenyl, naphthyl or heterocyclic radical, these latter three radicals optionally comprising one or more substituents selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy radicals and halogen atoms, process which comprises the treatment of an α-monohalogenated ketone of general formula: STR2 in which R and Cy have the same meaning as above and X represents chlorine, bromine or iodine, in the presence of an aqueous solution of an alkali metal hydroxide, a non-polar organic solvent selected from an aromatic or alicyclic hydrocarbon and oxygen in excess optionally in the presence of an inert gas, the treatment being carried out at a temperature ranging from the boiling temperature of the reaction medium at atmospheric pressure and 240° C. under pressure and the alkali metal so formed is then acidified to obtain the desired acid.