100757-90-2

Upstream product

• 78-77-3 Isobutyl bromide 
• 123-11-5 4-methoxy-benzaldehyde 
• 201230-82-2 carbon monoxide 
• 696-62-8 para-iodoanisole 
• 100-99-2 triisobutylaluminum 
• 82938-20-3 3-methyl-1-(4-methoxyphenyl)-1-butanone 
• 926-62-5 isobutylmagnesium bromide 
• 13139-86-1 4-methoxyphenyl magnesium bromide 
• 590-86-3 isovaleraldehyde 
• 104-92-7 1-bromo-4-methoxy-benzene 

Downstream Products

• 725233-70-5 C₁₂H₁₇ClO 
• 82938-20-3 3-methyl-1-(4-methoxyphenyl)-1-butanone 

Relevant academic research and scientific papers

Aminophenone compounds as well as preparation method and application thereof

The invention belongs to the technical field of medicinal chemistry, and particularly relates to aminophenone compounds as well as a preparation method and application thereof. The aminophenone compounds provided by the invention have a good inhibition effect on PDE4, also have good bioavailability, can be applied to preparation of drugs for treating PDE4-related diseases, and increase the optionsof drugs for treating PDE4-related diseases; and the effect of a part of the aminophenone compounds is equivalent to the effect of positive drugs, and the aminophenone compounds have good developmentpotential.

Enantioselective Oxy-Heck–Matsuda Arylations: Expeditious Synthesis of Dihydrobenzofuran Systems and Total Synthesis of the Neolignan (?)-Conocarpan

This work discloses the first examples of an effective enantioselective oxy-Heck–Matsuda reaction using a variety of styrenic olefins to generate chiral dihydrobenzofurans. The reaction proceeds in moderate to good yields, with high trans diastereoselectivity (up to 20:1) in enantioselectivities up to 90:10 using the N,N-ligand pyrimidine-bisoxazoline (PyriBox). The oxy-Heck–Matsuda reactions were carried out under mild conditions and rather low catalyst loadings. The feasibility and practicality of the process is demonstrated by a concise total synthesis of the neolignan (?)-conocarpan. X-ray diffraction of an advanced brominated intermediate in the route to (?)-conocarpan has allowed the unequivocal assignment of the absolute stereochemistry of the oxy-Heck–Matsuda aryldihydrobenzofuran products. A rationale for the mechanism operating in these enantioselective oxy-Heck–Matsuda reactions is also presented. (Figure presented.).

3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. Part 2: Optimization of the side chains to improve in vitro and in vivo potencies

A series of 3-[2-{[(3-methyl-1-phenylbutyl)amino]carbonyl}-4-(phenoxymethyl)phenyl]propanoic acid analogs were synthesized and evaluated for their in vitro potency. In most cases, introduction of one or two substituents into the two phenyl moieties resulted in the tendency of an increase or retention of in vitro activities. Several compounds, which showed excellent subtype selectivity, were evaluated for their inhibitory effect against PGE2-induced uterine contraction in pregnant rats, which is thought to be mediated by the EP3 receptor subtype. The structure-activity relationships (SARs) are also discussed.

Direct C-allylation of aryl-alkyl/glycosyl carbinols: Facile synthesis of C-linked carbo-β2-/γ2-/δ2- amino acids

A facile ZrCl4-catalyzed direct allylation of the p-methoxyphenyl-alkyl/glycosyl carbinols at room temperature, and the conversion of the derived aryl-glycosyl-alkenes into hitherto unknown C-linked carbo-β2-/γ2-/δ2-amino acids is reported.

Influence of Alkyl Chain Ramification on Estradiol Receptor Binding Affinity and Intrinsic Activity of 1,2-Dialkylated 1,2-Bis(4- or 3-hydroxyphenyl)ethane Estrogens and Antiestrogens

The influence of a symmetrical introduction of CH3 substituents in the α or β positions of the 1,2-dialkyl-1,2-bis(4-hydroxyphenyl)ethene estrogens hexestrol (ethyl, HES) and octestrol (n-propyl, OCES) isopropyl (1), tert-butyl (2), sec-butyl (3), isobut

CARBONYLATIVE CROSS-COUPLING REACTION OF ARYL IODIDES WITH ALKYLALUMINUMS BY PALLADIUM COMPLEX CATALYSIS

Secondary and/or tertiary alcohols and unsymmetrical ketones have been obtained in moderate to good yields by palladium-catalyzed (5 molpercent) carbonylative coupling of aryl iodides with alkylaluminum compounds under very mild conditions (20-50 deg C, 1 atm of carbon monoxide).The type of th reaction product depended on the aluminum reagent employed.While the selective formation of secondary alcohols was observed in the reaction with i-Bu3Al, the use of Et3Al led to a mixture of a ketone and two alcoholic products.With Et2AlCl predominantly unsymmetrical ketones were produced.In all cases, formation of directly cross-coupled products was not observed.DME and benzene can be used as solvents, but THF is unsuitable.Nickel catalysts were found to be ineffective for this reaction.