131002-03-4

Upstream product

• 42872-73-1 4-methyl-2-bromobenzonitrile 
• 53456-09-0 4-methyl-2-bromobenzoyl chloride 
• 7697-27-0 2-bromo-4-methylbenzoic acid 
• 103286-27-7 2-bromo-4-methylacetophenone 
• 42872-83-3 2-bromo-5-methylbenzylnitrile 
• 619-55-6 para-methylbenzamide 

Downstream Products

• 131002-07-8 2-ethenyl-4-methylbenzamide 
• 131002-10-3 6-methyl-2H-isoquinolin-1-one 
• 42872-73-1 4-methyl-2-bromobenzonitrile 
• 39549-79-6 2-amino-4-methylbenzamide 
• 1269219-55-7 7-methyl-2-(4-methoxyphenyl)quinazolin-4(3H)-one 
• 1293323-97-3 2-bromo-4-methylbenzylamine hydrochloride 
• 1293324-10-3 (2-bromo-4-methylbenzyl)(cyclohex-2-enyl)carbamic acid tert-butyl ester 
• 4337-47-7 6-methylbenzo[d]isothiazol-3(2H)-one 
• 155694-70-5 6-methyl-3-phenylisoquinolin-1(2H)-one 
• 619-55-6 para-methylbenzamide 
• 1177559-17-9 4-(aminomethyl)-2-bromobenzonitrile hydrochloride 
• 1177558-38-1 2-bromo-4-((1,3-dioxoisoindolin-2-yl)methyl)benzonitrile 
• 89892-38-6 2-bromo-4-(bromomethyl)benzonitrile 
• 1208076-70-3 C₈H₈BrNS 

Relevant academic research and scientific papers

NEUROPROTECTIVE PDI MODULATING SMALL MOLECULES AND METHODS OF USE THEREOF

The present disclosure provides, inter alia, compounds and compositions having the formula (I) as defined herein. Methods of using and making such compounds and compositions are also provided. The present disclosure further provides screening methods, including detectable probes as well as diagnostic methods and methods for monitoring the progress of a disease, such as a neurodegenerative disease.

Acid-promoted palladium(II)-catalyzed ortho-halogenation of primary benzamides: En route to halo-arenes

Br?nsted acid-promoted palladium(II)-catalyzed regioselective installation of halogens (Br, Cl, and I) to the aromatic ring of benzamide derivatives has been achieved using primary amides. A wide variety of benzamides were compatible under established conditions to afford the halogenated products without installing any external auxiliary. Mild reaction conditions, use of primary amide as a directing group, external additive-free conditions, and gram-scale reaction are some appealing features of this protocol. Detailed experimental results revealed that Br?nsted acid plays a critical role in this transformation.

Nickel-catalyzed regioselective C-H halogenation of electron-deficient arenes

A straightforward Ni(ii)-catalyzed general strategy was developed for the ortho-halogenation of electron-deficient arenes with easily available halogenating reagents N-halosuccinimides (NXS; X = Br, Cl and I). The transformation was highly regioselective and a wide substrate scope and functional group tolerance were observed. This discovery could be of great significance for the selective halogenation of amides, benzoic esters and other substances with guiding groups. Mechanistic investigations were also described.

Transfer Hydro-dehalogenation of Organic Halides Catalyzed by Ruthenium(II) Complex

A simple and efficient Ru(II)-catalyzed transfer hydro-dehalogenation of organic halides using 2-propanol solvent as the hydride source was reported. This methodology is applicable for hydro-dehalogenation of a variety of aromatic halides and α-haloesters and amides without additional ligand, and quantitative yields were achieved in many cases. The potential synthetic application of this method was demonstrated by efficient gram-scale transformation with catalyst loading as low as 0.5 mol %.

TBAI-catalyzed oxidative synthesis of benzamides from acetophenones and carbinols

An interesting and convenient procedure for the oxidative transformation of acetophenones and carbinols to primary benzamides has been developed. By using tetra-n-butylammonium iodide (TBAI) as the catalyst and tert-butyl hydroperoxide (TBHP) as the oxidant, the desired benzamides were isolated in moderate to good yields in aqueous solution. Notably, not only acetophenones but also propiophenones can be applied as substrates as well. Hence, we believe that this new procedure is not just a catalytic version of the iodine-based method. the Partner Organisations 2014.

Rapid synthesis and zebrafish evaluation of a phenanthridine-based small molecule library

A Heck cyclisation approach is described for the rapid synthesis of a library of natural product-like small molecules, based on the phenanthridine core. The synthesis of a range of substituted benzylamine building blocks and their incorporation into the library is reported, together with a highly selective cis-dihydroxylation protocol that enables access to the target compounds in an efficient manner. Biological evaluation of the library using zebrafish phenotyping has led to the discovery of compound 20c, a novel inhibitor of early-stage zebrafish embryo development.

Dual Pharmacophores - PDE4-Muscarinic Antagonistics

The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.

DUAL PHARMACOPHORES - PDE4-MUSCARINIC ANTAGONISTICS

The present invention is directed to novel compounds of Formula's (I) - (VI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of and/or prophylaxis of respiratory diseases, including inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.

Dual Pharmacophores - PDE4-Muscarinic Antagonistics

The present invention is directed to novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use as dual chromaphores having inhibitory activity against PDE4 and muscarinic acetylcholine receptors (mAChRs), and thus being useful for treating respiratory diseases.

Dual Pharmacophores - PDE4-Muscarinic Antagonistics

The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.