4133-35-1

Usage

Chemical Properties

pale yellow to brown crystalline powder

InChI:InChI=1/C10H9BrO/c11-9-3-1-8-6-10(12)4-2-7(8)5-9/h1,3,5H,2,4,6H2

Upstream product

• 37859-24-8 2-(4-bromophenyl)acetyl chloride 
• 74-85-1 ethene 
• 1878-68-8 2-(4-bromophenyl)-acetic acid 
• 79-37-8 oxalyl dichloride 

Downstream Products

• 659736-46-6 3',4'-dihydro-6'-bromo-spiro[imidazolidine-4,2'(1'H)-naphthalene]-2,5-dione 
• 136081-50-0 6-oxo-5,6,7,8-tetrahydronaphthalene-2-carbonitrile 
• 912953-53-8 6-[4-(trifluoromethyl)phenyl]-3,4-dihydro-2(1H)-naphthalenone 
• 113075-66-4 1-(6-bromo-3,4-dihydro-2-naphthyl)pyrrolidine 
• 1062649-18-6 6-p-tolyl-3,4-dihydronaphthalen-2(1H)-one 
• 418772-22-2 1-(1-(RS)-benzyl-6-bromo-3,4-dihydro-1H-naphthalen-2-ylidene)-pyrrolidinium bromide 
• 863925-41-1 N-benzyl-6-bromo-1,2,3,4-tetrahydronaphthalen-2-amine 
• 740842-87-9 7-bromo-2,3,4,5-tetrahydro-1H-benzo[c]azepine 
• 740842-86-8 7-bromo-2,3,4,5-tetrahydro-1H-benzo[d]azepine 
• 740842-89-1 tert-butyl 7-bromo-2,3,4,5-tetrahydro-2H-benzo[c]azepine-2-carboxylate 
• 740842-88-0 tert-butyl 7-bromo-1,2,4,5-tetrahydro-3H-benzo[d]azepine-3-carboxylate 
• 1345098-51-2 (1S)-2,3,5,6-tetrahydro-8-bromo-1-phenyl-1H-benzo[f]chromen-3-ol 

Relevant academic research and scientific papers

Discovery and Development of Metal-Catalyzed Coupling Reactions in the Synthesis of Dasabuvir, an HCV-Polymerase Inhibitor

Dasabuvir (1) is an HCV polymerase inhibitor which has been developed as a part of a three-component direct-acting antiviral combination therapy. During the course of the development of the synthetic route, two novel coupling reactions were developed. First, the copper-catalyzed coupling of uracil with aryl iodides, employing picolinamide 16 as the ligand, was discovered. Later, the palladium-catalyzed sulfonamidation of aryl nonaflate 33 was developed, promoted by electron-rich palladium complexes, including the novel phosphine ligand, VincePhos (50). This made possible a convergent, highly efficient synthesis of dasabuvir that significantly reduced the mutagenic impurity burden of the process.

1-(DIHYDRONAPHTHALENYL)PYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS

Provided are 1-(dihydronaphthalenyl)pyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy for the treatment of obesity and diabetes.

1-(DIHYDRONAPHTHALENYL)PYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS

This invention relates to novel 1-(dihydronaphthalenyl)pyridones which are antagonists of the melanin-concentrating hormone receptor 1 (MCHR1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy

PHENANTHRENONE COMPOUNDS, COMPOSITIONS AND METHODS

The present invention is directed to compounds of Formula (I) or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.

Tricyclic Compound, Compositions, and Methods

The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.

Heteroaryl β-tetralin ureas as novel antagonists of human TRPV1

We report on a series of α-substituted-β-tetralin-derived and related phenethyl-based isoquinolinyl and hydroxynaphthyl ureas as potent antagonists of the human TRPV1 receptor. The synthesis and Structure-activity relationships (SAR) of the series are described.

Novel ligands for the human histamine H1 receptor: Synthesis, pharmacology, and comparative molecular field analysis studies of 2-dimethylamino-5-(6)-phenyl-1,2,3,4-tetrahydronaphthalenes

This paper reports the synthesis of a novel series of (±)-2-dimethylamino- 5- and 6-phenyl-1,2,3,4-tetrahydronaphthalene derivatives (5- and 6-APTs), and, corresponding affinity, functional activity, and, molecular modeling studies with regard to drug des

Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH2 at the human melanocortin-1 and -4 receptors: Histidine substitution

Systematic substitution of His6 residue using non-selective hMC4R pentapeptide agonist (Bu-His6-DPhe7-Arg8-Trp9-Gly 10-NH2) as the template led to the identification of Bu-Atcsu

Glucocorticoid receptor modulators

The present invention provides non-steroidal compounds of Formula I, and prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds.

Pharmaceutically active benzoquinazoline compounds

Compounds of formula (I) or salts thereof, wherein the dotted line represents a single or double bond, R1is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4and R5are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8wherein n is the integer 0, 1 or 2 and R8is halo or alkyl or a group NR9R10wherein R9and R10are both hydrogen, a group NR11R12wherein R11and R12are the same or different and each is hydrogen or alkyl, a group OR13wherein R13is hydrogen or C1-4alkyl optionally substituted by halo; a C1-4aliphatic group optionally substituted by a group OR14or NR14R15wherein R14and R15are the same or different and each is hydrogen or alkyl; or two of R2to R5are linked together to form a benzo group, or one of R2to R5is a group -X-Y-R16wherein X is CH2, NR17, CO or S(O)m, and Y is CH2, NR17, O, or S(O)m, or -X-Y- is a group -O-, -NR17-, -CH=CH- or -N=N-, are disclosed as pharmacological agents useful in the treatment of tumours. Pharmaceutical compositions and methods for the preparation of compounds of formula (I) are also described.