807667-27-2

Upstream product

• 20401-88-1 3-(4-methoxyphenyl)propional 
• 1929-29-9 3-(4-methoxyphenyl)propanoic acid 
• 104-94-9 4-methoxy-aniline 
• 53484-50-7 (E)-p-methoxy-cinnamyl alcohol 
• 107-02-8 acrolein 
• 4346-59-2 para-methoxyphenyldiazonium chloride 

Downstream Products

• 304895-28-1 N-[5-(4-methoxybenzyl)-1,3-thiazol-2-yl]heptanamide 
• 1029712-74-0 2-(4-fluorophenyl)-7-(4-methoxybenzyl)imidazo[1,2-b][1,2,4]triazine 
• 1029712-77-3 6-(4-fluorophenyl)-3-(4-methoxybenzyl)imidazo[1,2-a]pyrimidine 
• 304895-22-5 2-chloro-N-[5-[(4-methoxyphenyl)methyl]thiazol-2-yl]acetamide 
• 1267970-83-1 4-((2-(4-(4-methoxybenzyl)thiazol-2-yl)hydrazono)methyl)benzene-1,3-diol 

Relevant academic research and scientific papers

Synthesis and BK channel-opening activity of 2-amino-1,3-thiazole derivatives

A series of 2-amino-5-arylmethyl- or 5-heteroarylmethyl-1,3-thiazole derivatives were synthesized and evaluated for BK channel-opening activities in cell-based fluorescence assay and electrophysiological recording. The assay results indicated that the activities of the investigated compounds were influenced by the physicochemical properties of the substituent at benzene ring.

Synthesis and anticancer properties of n-(5-r-benzyl-1,3-thiazol-2-yl)-2,5-dimethyl-3-furamides

Aim. Study of the synthesis and anticancer activity of a series of N-(5-R-benzyl-1,3-thiazol-2-yl)-2,5-dimethyl-3-furamides. Methods. Organic synthesis, analytical and spectral methods, pharmacological screening. Results. N-(5-R-benzyl-1,3-thiazol-2-yl)-2

Carbene-Catalyzed α-Carbon Amination of Chloroaldehydes for Enantioselective Access to Dihydroquinoxaline Derivatives

An NHC-catalyzed α-carbon amination of chloroaldehydes was developed. Cyclohexadiene-1,2-diimines are used as amination reagents and four-atom synthons. Our reaction affords optically enriched dihydroquinoxalines that are core structures in natural products and synthetic bioactive molecules.

N-Heterocyclic Carbene-Catalyzed Synthesis of α-Trifluoromethyl Esters

The N-heterocyclic carbene (NHC)-catalyzed trifluoromethylation of α-chloro aldehydes was developed, allowing straightforward access to valuable α-trifluoromethyl ester derivatives. The unique combination of an electrophilic trifluoromethylation reagent with NHC catalysis was the key for the functionalization of a broad range of α-chloro aldehydes, and the products are formed in moderate to good yields. Investigations of the enantioselective version of this reaction afforded the enantioenriched products in moderate yields with good ee values.

Trifluoromethylthiolation of α-Chloroaldehydes: Access to Quaternary SCF3-Containing Centers

In this study, a straightforward methodology was developed to access quaternary α-trifluoromethylthiolated chloroaldehydes. Using the Munavalli reagent as the electrophilic SCF3 source, a base-catalyzed trifluoromethylthiolation reaction with a panel of α-chloroaldehydes was successfully achieved under mild reaction conditions. The α-trifluoromethylthiolated chloroaldehydes were obtained in moderate to high yields (up to 88 %). This approach demonstrated a good functional-group tolerance and offered access to highly functionalized quaternary trifluoromethylthiolated aldehydes, inaccessible so far. The development of an enantioselective version was investigated by using a chiral phase-transfer catalyst, giving the enantioenriched product in moderate enantiomeric excess.

Synthesis and antitumor activities of new n-(5-benzylthiazol-2-yl)-2-(heteryl-5-ylsulfanyl)-acetamides

Aim. Synthesis of a series of new N-(5-benzyl-thiazol-2-yl)-2-(heteryl-5-ylsulfanyl)-acetamides and study of their anticancer activity. Methods. Organic synthesis, analytical and spectral methods, pharmacological screening. Results. [2-chloro-N-(5-aryl-1,

Aminothiazoles as Potent and Selective Sirt2 Inhibitors: A Structure-Activity Relationship Study

Sirtuins are NAD+-dependent protein deacylases that cleave off acetyl but also other acyl groups from the ε-amino group of lysines in histones and other substrate proteins. Dysregulation of human Sirt2 (hSirt2) activity has been associated with the pathogenesis of cancer, inflammation, and neurodegeneration, which makes the modulation of hSirt2 activity a promising strategy for pharmaceutical intervention. The sirtuin rearranging ligands (SirReals) have recently been discovered by us as highly potent and isotype-selective hSirt2 inhibitors. Here, we present a well-defined structure-activity relationship study, which rationalizes the unique features of the SirReals and probes the limits of modifications on this scaffold regarding inhibitor potency. Moreover, we present a crystal structure of hSirt2 in complex with an optimized SirReal derivative that exhibits an improved in vitro activity. Lastly, we show cellular hyperacetylation of the hSirt2 targeted tubulin caused by our improved lead structure.

Iridium-catalyzed 1,3-hydrogen shift/chlorination of allylic alcohols

Tandem: Allylic alcohols react with N-chlorosuccinimide (NCS) in a tandem 1,3-H shift/C-Cl bond formation leading to α-chloroketones and α-chloroaldehydes. The reactions proceed with complete selectivity to give single constitutional isomers of monochlorinated carbonyl compounds. The utility of the transformation is illustrated by the straightforward synthesis of 4,5-disubstituted 2-aminothiazoles from allylic alcohols. Copyright

ENHANCERS OF PROTEIN DEGRADATION

The present invention relates to compounds suitable for modulating huntingtin protein processing and useful for treating or preventing huntingtin-related disorders. The invention provides pharmaceutical compositions comprising said compounds and methods of syntheses thereof.

Discovery and potency optimization of 2-amino-5-arylmethyl-1,3-thiazole derivatives as potential therapeutic agents for prostate cancer

A new chemical series was identified via high-throughput screening as having antiproliferative activity on DU-145 human prostate carcinoma cell line (hit compound potency - 2.9 μM). Medicinal chemistry optimization of two peripheral diversity vectors of t