332-42-3

Usage

Uses

Used in Pharmaceutical Industry:
1-(2-BROMOETHYL)-4-FLUOROBENZENE is used as a key intermediate in the production of protein A mimetics, which are engineered proteins that mimic the binding properties of natural protein A. These mimetics have potential applications in various therapeutic and diagnostic areas, such as antibody purification, immunoassays, and drug delivery systems.
Used in Pharmaceutical Industry:
1-(2-BROMOETHYL)-4-FLUOROBENZENE is also utilized as an intermediate in the synthesis of serotonin antagonists, which are drugs that block the action of serotonin, a neurotransmitter involved in various physiological processes. These antagonists have potential applications in the treatment of disorders such as depression, anxiety, and obsessive-compulsive disorder.
Used in Pharmaceutical Industry:
Furthermore, 1-(2-BROMOETHYL)-4-FLUOROBENZENE is employed as an intermediate in the development of other central nervous system (CNS) agents. These agents can have various therapeutic applications, such as treating neurological disorders, pain management, and cognitive enhancement.

Upstream product

• 7589-27-7 2-(4-Fluorophenyl)ethanol 
• 6529-53-9 1-(2-bromoethyl)-4-chlorobenzene 
• 90867-08-6 4-Fluoro-α-ethylbenzenium ion 
• 7789-60-8 phosphorus tribromide 
• 497-19-8 sodium carbonate 
• 405-99-2 para-fluorostyrene 
• 70931-33-8 1-[2-(4-fluorophenyl)-ethyl]-piperazine 
• 70931-13-4 11-chloro-7-fluoro-2-isopropyl-10,11-dihydrodibenzothiepin 
• 352-13-6 4-flourophenylmagnesium bromide 
• 405-50-5 p-Fluorophenylacetic acid 

Downstream Products

• 405-99-2 para-fluorostyrene 
• 1583-88-6 4-fluoro-2-phenethylamine 
• 459-28-9 N-methyl-N-[2-(4-fluoro-phenyl)-ethyl]-amine 
• 54540-67-9 1-(3,5-Dimethoxyphenyl)-4-(4-fluorphenyl)-2-methyl-butan-1-on 
• 54540-82-8 2-(3,5-Dimethoxyphenyl)-4-(4-fluorphenyl)-butan 
• 52059-52-6 N-Methyl-β-(p-fluorphenyl)-β'-phenyl-diaethylamin 
• 70931-36-1 1-ethoxycarbonyl-4-<2-(4-fluorophenyl)ethyl>piperazine 
• 175553-31-8 1-[2-(4-fluorophenyl)-ethyl]-piperidine-4-carboxylic acid ethyl ester 
• 6529-53-9 1-(2-bromoethyl)-4-chlorobenzene 
• 90867-08-6 4-Fluoro-α-ethylbenzenium ion 
• 258513-99-4 4-(4-fluorophenethoxy)phenyl benzyl ether 
• 259268-47-8 N-(4-fluorophenylethyl)-3-piperidinecarboxamide 
• 259268-44-5 [1-(2-benzhydryloxy-ethyl)-piperidin-3-ylmethyl]-[2-(4-fluoro-phenyl)-ethyl]-amine 
• 139290-65-6 R-(+)-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol 

Relevant academic research and scientific papers

Cascade bio-hydroxylation and dehalogenation for one-pot enantioselective synthesis of optically active β-halohydrins from halohydrocarbons

A stereoselective hydroxylation and enantioselective dehalogenation cascade reaction was developed for the synthesis of optically active β-haloalcohols from halohydrocarbons. This cascade system employed P450 and halohydrin dehalogenase as two compatible biocatalysts, allowing a straightforward, greener and efficient access to β-halohydrins with excellent enantioselectivities (98-99%).

Scalable anti-Markovnikov hydrobromination of aliphatic and aromatic olefins

To improve access to a key synthetic intermediate we targeted a direct hydrobromination-Negishi route. Unsurprisingly, the anti-Markovnikov addition of HBr to estragole in the presence of AIBN proved successful. However, even in the absence of an added initiator, anti-Markovnikov addition was observed. Re-examination of early reports revealed that selective Markovnikov addition, often simply termed "normal" addition, is not always observed with HBr unless air is excluded, leading to the rediscovery of a reproducible and scalable initiator-free protocol.

Spiroalkene carboxamide derivatives and their use as chemokine receptor modulators

The present invention is directed to compounds of Formula (I) below, which are antagonists to the chemoattractant cytokine receptor 2 (CCR2), and/or 5 (CCR5), pharmaceutical compositions, and methods for use thereof.

SPIROALKENE CARBOXAMIDE DERIVATIVES AND THEIR USE AS CHEMOKINE RECEPTOR MODULATORS

The present invention is directed to compounds of Formula (I) below, which are antagonists to the chemoattractant cytokine receptor 2 (CCR2), and/or 5 (CCR5), pharmaceutical compositions, and methods for use thereof.

3-Hydroxypyrimidine-2,4-diones as an Inhibitor Scaffold of HIV Integrase

Integrase (IN) represents a clinically validated target for the development of antivirals against human immunodeficiency virus (HIV). Inhibitors with a novel structure core are essential for combating resistance associated with known IN inhibitors (INIs). We have previously disclosed a novel dual inhibitor scaffold of HIV IN and reverse transcriptase (RT). Here we report the complete structure-activity relationship (SAR), molecular modeling, and resistance profile of this inhibitor type on IN inhibition. These studies support an antiviral mechanism of dual inhibition against both IN and RT and validate 3-hydroxypyrimidine-2,4-diones as an IN inhibitor scaffold.

Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET

Radiolabelled piperidine derivatives such as [11C]MDL 100907 and [18F]altanserin have played an important role in diagnosing malfunction in the serotonergic neurotransmission. A variety of novel piperidine MDL 100907 derivatives, possible to label with 18F-fluorine, were synthesized to improve molecular imaging properties of [11C]MDL 100907. Their in vitro affinities to a broad spectrum of neuroreceptors and their lipophilicities were determined and compared to the clinically used reference compounds MDL 100907 and altanserin. The novel compounds MA-1 (53) and (R)-MH.MZ (56) show Ki-values in the nanomolar range towards the 5-HT2A receptor and insignificant binding to other 5-HT receptor subtypes or receptors. Interestingly, compounds MA-1 (53), MH.MZ (55) and (R)-MH.MZ (56) provide a receptor selectivity profile similar to MDL 100907. These compounds could possibly be preferable antagonistic 18F-tracers for visualization of the 5-HT2A receptor status. Medium affine compounds (VK-1 (32), (51), (52), (54)) were synthesized and have Ki values between 30 and 120 nM. All promising compounds show log P values between 2 and 3, that is, within the range of those for the established radiotracers altanserin and MDL 100907. The novel compounds MA-1 (53) and (R)-MH.MZ (56) thus appear to be promising high affine and selective tracers of 18F-labelled analogues for 5-HT2A imaging with PET.

Total synthesis and evaluation of [18F]MHMZ

Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[18F]fluoroethyltosylate ([18F]FETos) was carried out in yields of ～90% synthesizing [18F]MHMZ in a specific activity of ～50 MBq/nmol with a sta

2 -ALKYL- INDAZOLE COMPOUNDS FOR THE TREATMENT OF CERTAIN CNS-RELATED DISORDERS

2-Alkyl-indazole compound and its pharmaceutically acceptable salts of acid addition, method and intermediates for preparing them, a pharmaceutical composition containing them and use of the latter. The 2-alkyl-indazole compound has the following general formula (I) in which R1, R2, R3, R4, R6, R7, X, Y, W, n, p, and m have the meanings stated in the description.

Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-substituted phenyl alkyl imidazole-based inhibitors of the enzyme complex 17α-hydroxylase/17,20-lyase (P45017α)

We report the preliminary results of the synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a number of phenyl alkyl imidazole-based compounds as inhibitors of the two components of 17α-hydroxylase/17,20-lyase (P45017α), that is, 17α-hydroxylase (17α-OHase) and 17,20-lyase (lyase). The results show that N-3-(4-bromophenyl) propyl imidazole (12) (IC50 = 2.95 μM against 17α-OHase and IC50 = 0.33 μM against lyase) is the most potent compound within the current study, in comparison to ketoconazole (KTZ) (IC50 = 3.76 μM against 17α-OHase and IC50 = 1.66 μM against lyase). Modelling of these compounds suggests that the length of the alkyl chain enhances the interaction between the inhibitor and the area of the active site corresponding to the C(3) area of the steroid backbone, thereby increasing potency.

The "reverse-tethered" ruthenium (II) catalyst for asymmetric transfer hydrogenation: Further applications

The attachment of a tethering group from the basic nitrogen atom to the arene ligand of a ruthenium(II) catalyst greatly improves its ability to catalyze asymmetric transfer hydrogenation (ATH) reactions. In this paper, we describe further applications of this versatile system to an extended substrate range.