87282-25-5

Upstream product

• 100-39-0 benzyl bromide 
• 142501-48-2 (3,4,5-trimethoxyphenyl)(trimethylsilyloxy)acetonitrile 
• 10028-15-6 ozone 
• 64-19-7 acetic acid 
• 208347-79-9 1-(3,4,5-trimethoxyphenyl)-2-phenylacetylene 
• 86-81-7 3,4,5-trimethoxy-benzaldehyde 
• 1916-07-0 3,4,5-trimethoxybenzoic acid methyl ester 
• 860764-83-6 1,3-diphenyl-2-(3,4,5-trimethoxy-phenyl)-propan-2-ol 
• 1589-82-8 phenylmagnesium bromide 
• 133462-61-0 2-phenyl-1-(3,4,5-trimethoxyphenyl)ethanol 
• 140-29-4 phenylacetonitrile 
• 182163-96-8 3,4,5-trimethoxyphenylboronic Acid 

Downstream Products

• 1202168-41-9 (E)-1-(3,4,5-trimethoxyphenyl)-3-(4-methoxyphenyl)-2-phenylprop-2-en-1-one 

Relevant academic research and scientific papers

Novel diaryl-2H-azirines: Antitumor hybrids for dual-targeting tubulin and DNA

Multiple-target drugs may achieve better therapeutic effect via different pathways than single-target ones, especially for complex diseases. Tubulin and DNA are well-characterized molecular targets for anti-cancer drug development. A novel class of diaryl substituted 2H-azirines were designed based on combination of pharmacophores from Combretastatin A-4 (CA-4) and aziridine-type alkylating agents, which are known tubulin polymerization inhibitor and DNA damaging agents, respectively. The antitumor activities of these compounds were evaluated in vitro and 6h showed the most potent activities against four cancer cell lines with IC50 values ranging from 0.16 to 1.40 μM. Further mechanistic studies revealed that 6h worked as a bifunctional agent targeting both tubulin and DNA. In the nude mice xenograft model, 6h significantly inhibited the tumor growth with low toxicity, demonstrating the promising potential for further developing novel cancer therapy with a unique mechanism.

Coupling of Sulfoxonium Ylides with Arynes: A Direct Synthesis of Pro-Chiral Aryl Ketosulfoxonium Ylides and Its Application in the Preparation of α-Aryl Ketones

A general, mild, and versatile synthesis of the challenging α-aryl-β-ketosulfoxonium ylides has been developed for the first time, substituting traditional methods starting from diazo compounds. The arylation of easily accessible β-ketosulfoxonium ylides using aryne chemistry allowed the preparation of a large scope of the pro-chiral ylides in very good yields (40 examples; up to 85%). As applications, these ylides were smoothly converted into α-aryl ketones after desulfurization in good yields (up to 98%) as well as in other important derivatives.

Efficient synthesis of alkyl aryl ketones & ketals via palladium-catalyzed regioselective arylation of vinyl ethers

The combination of Pd(OAc)2 with 1,3-bis(diphenylphosphino) propane (dppp) in ethylene glycol constitutes a high-performance catalytic system for highly regioselective arylation of a range of electron-rich vinyl ethers by aryl bromides to provide, upon hydrolysis, alkyl aryl ketones and cyclic ketals in good yields with up to 3.75 × 105 TON and 15625 h-1 TOF.

p-Toluenesulfonic acid-promoted selective functionalization of unsymmetrical arylalkynes: a regioselective access to various arylketones and heterocycles

Regioselective hydration of a wide range of internal alkynes has been afforded in high to good yields by using PTSA in EtOH. The scope of the reaction of alkynes has been delineated. Arylaliphatic alkynes and diarylalkynes were regioselectively hydrated in good to excellent yields and short reaction times when the reaction was achieved under microwave irradiation. Moreover, diarylalkynes, arylenynes as well as diaryldiynes bearing a methoxy- or a thiomethyl substituent on the ortho position underwent a regioselective 5-endo-dig-cyclization to give a variety of 2-aryl- and 2-styrylbenzofuran or benzothiphene derivatives. We believe that, this new environmentally metal-free procedure combined to microwave irradiation would be in importance in the search of green laboratory-scale synthesis.

Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones

Tubulin is an important molecular target in cancer chemotherapy. Antimitotic agents able to bind to the protein are currently under study, commonly used in the clinic to treat a variety of cancers and/or exploited as probes to investigate the protein's st

Rapid microwave assisted hydration of internal arylalkynes in the presence of PTSA: an efficient regioselective access to carbonyl compounds

A metal-free procedure for the regioselective hydration of internal arylalkynes under microwave irradiation is described. The reaction promoted by PTSA takes place rapidly in EtOH and regioselectively afforded in good yields various carbonyl compounds 2.

Propenone derivatives

The present invention relates to propenone derivatives represented by the following formula (I): STR1 wherein R1 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, or YR5 (wherein Y represents S or O; and R5 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a substituted or unsubstituted cyclic ether residue); R2 and R3 independently represent hydrogen, lower alkyl, or substituted or unsubstituted aralkyl, or alternatively R2 and R3 are combined to form substituted or unsubstituted methylene or ethylene; R4 represents hydrogen, hydroxy, lower alkyl, substituted or unsubstituted aralkyl, lower alkoxy, substituted or unsubstituted aralkyloxy, or halogen; and X represents substituted or unsubstituted indolyl; or pharmaceutically acceptable salts thereof.

Intramolecular Oxidative Coupling of Aromatic Compounds. I Oxidation of Diphenolic Substrates

The synthesis of (2RS,3SR)-1-(3,5-dihydroxy-4-methoxyphenyl)-(4-hydroxy-3,5-dimethoxyphenyl)2,3-dimethylbutan-1-one (26) is described.Diphenolic oxidative coupling of (26) did not produce a eupodienone-type product.An aryltetralin derivative was formed in