1361414-32-5

Usage

Chemical compound

2-[4-(2-bromoacetyl)phenyl]ethyl acetate

Structure

derivative of acetate with an ethyl group and a phenyl group connected by a bromine-substituted acetyl group

Uses

commonly used in organic synthesis as a building block for pharmaceuticals, agrochemicals, and fine chemicals; also used as a flavor and fragrance agent in perfume and cosmetic products

Hazardous nature

presence of bromine group makes it potentially hazardous

Safety precautions

proper handling and storage measures should be taken

Upstream product

• 73823-79-7 β-(4-acetylphenyl)ethyl acetate 
• 103-45-7 acetic acid phenethyl ester 

Downstream Products

• 1361414-34-7 2-{4-[(2-amino-4-phenyl-1,3-thiazol-5-yl)carbonyl]phenyl}ethyl acetate 
• 1361413-43-5 N-(4-(3-cyanophenyl)-5-{[4-(2-hydroxyethyl)phenyl]carbonyl}-1,3-thiazol-2-yl)-2-[4-(ethylsulfonyl)phenyl] acetamide 
• 1361414-36-9 2-(4-{[2-({[4-(ethylsulfonyl)phenyl]acetyl} amino)-4-phenyl-1,3-thiazol-5-yl]carbonyl}phenyl)ethyl acetate 
• 1361413-41-3 2-[4-(ethylsulfonyl)phenyl]-N-(5-{[4-(2-hydroxyethyl)phenyl]carbonyl}-4-phenyl-1,3-thiazol-2-yl)acetamide 
• 1361414-41-6 2-(4-{[2-amino-4-(3-cyanophenyl)-1,3-thiazol-5-yl]carbonyl}phenyl)ethyl acetate 

Relevant academic research and scientific papers

Synthesis and pharmacological evaluation of [18F]PBR316: a novel PET ligand targeting the translocator protein 18 kDa (TSPO) with low binding sensitivity to human single nucleotide polymorphism rs6971

Radiopharmaceuticals that target the translocator protein 18 kDa (TSPO) have been investigated with positron emission tomography (PET) to study neuroinflammation, neurodegeneration and cancer. We have developed the novel, achiral, 2-phenylimidazo[1,2-a]pyridine, PBR316 that targets the translocator protein 18 kDa (TSPO) that addresses some of the limitations inherent in current TSPO ligands; namely specificity in binding, blood brain barrier permeability, metabolism and insensitivity to TSPO binding in subjects as a result of rs6971 polymorphism. PBR316 has high nanomolar affinity (4.7-6.0 nM) for the TSPO, >5000 nM for the central benzodiazepine receptor (CBR) and low sensitivity to rs6971 polymorphism with a low affinity binders (LABs) to high affinity binders (HABs) ratio of 1.5. [18F]PBR316 was prepared in 20 ± 5% radiochemical yield, >99% radiochemical purity and a molar activity of 160-400 GBq μmol?1. Biodistribution in rats showed high uptake of [18F]PBR316 in organs known to express TSPO such as heart (3.9%) and adrenal glands (7.5% ID per g) at 1 h. [18F]PBR316 entered the brain and accumulated in TSPO-expressing regions with an olfactory bulb to brain ratio of 3 at 15 min and 7 at 4 h. Radioactivity was blocked by PK11195 and Ro 5-4864 but not Flumazenil. Metabolite analysis showed that radioactivity in adrenal glands and the brain was predominantly due to the intact radiotracer. PET-CT studies in mouse-bearing prostate tumour xenografts indicated biodistribution similar to rats with radioactivity in the tumour increasing with time. [18F]PBR316 showsin vitrobinding that is insensitive to human polymorphism and has specific and selectivein vivobinding to the TSPO. [18F]PBR316 is suitable for further biological and clinical studies.

NOVEL COMPOUNDS

Disclosed are retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.