72269-20-6

Upstream product

• 586-89-0 4-acetyl-benzoic acid 
• 62-53-3 aniline 
• 201230-82-2 carbon monoxide 
• 99-91-2 para-chloroacetophenone 
• 13329-40-3 4-Iodoacetophenone 
• 144-62-7 oxalic acid 
• 321906-51-8 C₈H₇IOZn 
• 103-71-9 phenyl isocyanate 
• 31076-84-3 4-acetylbenzoyl chloride 
• 38117-54-3 cyclopentadienyl iron(II) dicarbonyl dimer 
• 67-56-1 methanol 

Downstream Products

• 1606159-84-5 4-acetyl-N-(3-methylbut-2-en-1-yl)-N-phenylbenzamide 
• 929602-14-2 1-(4-(4-phenylquinolin-2-yl)phenyl)ethan-1-one 

Relevant academic research and scientific papers

Rhodium-Catalyzed Addition of Organozinc Iodides to Carbon-11 Isocyanates

Amides were prepared using rhodium-catalyzed coupling of organozinc iodides and carbon-11 (11C, t1/2 = 20.4 min) isocyanates. Nonradioactive isocyanates and sp3 or sp2 organozinc iodides generated amides in yields of 13%-87%. Incorporation of cyclotron-produced [11C]CO2 into 11C-amide products proceeded in yields of 5%-99%. The synthetic utility of the methodology was demonstrated through the isolation of [11C]N-(4-fluorophenyl)-4-methoxybenzamide ([11C]6g) with a molar activity of 267 GBq μmol-1 and 12% radiochemical yield in 21 min from the beginning of synthesis.

Anti-oligomerization sheet molecules: Design, synthesis and evaluation of inhibitory activities against α-synuclein aggregation

Aggregation of α-synuclein (α-Syn) play a key role in the development of Parkinson Disease (PD). One of the effective approaches is to stabilize the native, monomeric protein with suitable molecule ligands. We have designed and synthesized a series of sheet-like conjugated compounds which possess different skeletons and various heteroatoms in the two blocks located at both ends of linker, which have good π-electron delocalization and high ability of hydrogen-bond formation. They have shown anti-aggregation activities in vitro towards α-Syn with IC50 down to 1.09 μM. The molecule is found binding in parallel to the NACore within NAC domain of α-Syn, interfering aggregation of NAC region within different α-Syn monomer, and further inhibiting or slowing down the formation of α-Syn oligomer nuclei at lag phase. The potential inhibitor obtained by our strategy is considered to be highly efficient to inhibit α-Syn aggregation.

Supported Palladium Nanoparticles that Catalyze Aminocarbonylation of Aryl Halides with Amines using Oxalic Acid as a Sustainable CO Source

Polystyrene-supported palladium (Pd@PS) nanoparticles (NPs) have been used to catalyze the aminocarbonylation of aryl halides with amines using oxalic acid as a CO source for the first-time for the synthesis of amides. Furthermore, o-iodoacetophenones participated in amidation and cyclization reactions to give isoindolinones in a single step following a concerted approach. Oxalic acid has been used as a safe, environmentally benign and operationally simple ex situ sustainable CO source under double-layer-vial (DLV) system for different aminocarbonylation reactions. Catalyst stability under a CO environment is a challenging task, however, Pd@PS was found to be recyclable and applicable for a vast substrate scope avoiding regeneration steps. Easy handling of oxalic acid, additive and base-free CO generation, catalyst stability and effortless catalyst separation from the reaction mixture by filtration and introduce of DLV are the added advantages to make the overall process a sustainable approach.

Method for synthesizing amide compound through photocatalysis in water phase

The invention discloses a method for synthesizing an amide compound through photocatalysis in a water phase. The method comprises the following steps: putting catalysis amounts of a free radical initiator, an amine derivative, a carboxylic acid derivative, a phase transfer catalyst, an inorganic base and water into a reaction container, carrying out a reaction in a photocatalysis reaction instrument at certain power under a room temperature condition, after a certain time, carrying out extraction by using a small amount of ethyl acetate, and carrying out recrystallization, so as to obtain theamide compound, wherein the free radical initiator is eosin, methyl orange, sodium persulfate, ammonium persulfate or potassium peroxodisulfate, the phase transfer catalyst is tetrabutylammonium bromide, and the power of the photocatalytic reaction instrument is 5W. By adopting the method disclosed by the invention, toxic thionyl chloride or phosphorus oxychloride is not needed for a chlorinationreaction, water is adopted as a solvent, a novel photocatalysis method is used, and the amide compound with a high yield can be prepared through a room-temperature reaction for 2-5 hours with an incandescent light bulb of 5W, and in addition, the method is simple in aftertreatment, and low in cost and is an ideal green synthesis method of amide compounds.

SUBSTITUTED 5-(HALOALKYL)-5-HYDROXY-ISOXAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI

The present invention relates to 5-(haloalkyl)-5-hydroxy-isoxazoles of the formula (I), or the N-oxides, or the agriculturally useful salts thereof, and the use thereof for controlling phytopathogenic fungi; to a method for combating phytopathogenic harmf

Photoinduced Aminocarbonylation of Aryl Iodides

Transition metal-catalyzed aminocarbonylation of aryl halides with CO and amines, pioneered by Heck and co-workers in the 1970s, is among the most commonly employed reactions to make aromatic amides. A catalyst-free aminocarbonylation of aryl iodides with CO and amines, which simply uses photoirradiation conditions by Xe-lamp, has now been developed. This methodology shows broad functional-group tolerance, including that of heteroaromatic amides. A hybrid radical/ionic chain mechanism, involving electron transfer from zwitterionic radical intermediates generated by nucleophilic attack of amines to aroyl radicals, is proposed.

Aminocarbonylation of aryl iodides with primary and secondary amines in aqueous medium using polymer supported palladium-N-heterocyclic carbene complex as an efficient and heterogeneous recyclable catalyst

Aminocarbonylation of aryl iodides with primary and secondary aromatic/aliphatic amines to corresponding amides using polymer supported palladium-N-heterocyclic carbene complex (PS-Pd-NHC) as an efficient heterogeneous, recyclable catalyst is described. The catalytic system was optimized with respect to various reaction parameters to give excellent yield of desired products. The catalyst can be easily separated by simple filtration process and recycled further up to four consecutive recycle without loss in any activity and selectivity. The protocol is advantageous due to the ease in handling of the catalyst, simple workup procedure, and environmentally benign water as solvent and effective catalyst recyclability.

Bis(cyclopentadienyldicarbonyliron) as a convenient carbon monoxide source in palladium-catalyzed carbonylative coupling of aryl iodides with amines, alcohols, and thiols

Bis(cyclopentadienyldicarbonyliron) ([CpFe(CO)2]2) serves as a carbon monoxide source in carbonylative coupling reactions. Treatment of aryl iodides with primary amines in the presence of DBU and [CpFe(CO)2]2 under palladium catalysis provides the corresponding benzamides in good yields. Similar reactions with phenols and thiols provide the corresponding benzoate esters and thioesters, respectively. A catalytic amount of DMAP as an additive promoted the carbonylative coupling reactions with primary alcohol and secondary amine.

Method for Producing Aromatic and Heteroaromatic Carboxylic Acids, Carboxylic Acid Esters and Carboxylic Acid Amides

Process for the preparation of aromatic and heteroaromatic carboxylic acids, carboxylic acid esters and carboxamides by the reaction of aromatic or heteroaromatic halides R—Xn, in which n=integer from 1 to 6, R=substituted or unsubstituted and aromatic or heteroaromatic radical and X=chlorine, bromine or iodine atom, with carbon monoxide and water, ammonia, alcohols or amines in the presence of bases and zero-valent or divalent palladium compounds and bidentate diphosphanes or complexes of zero-valent or divalent palladium with bidentate diphosphanes, in which use is made of bidentate diphosphanes [in-line-formulae](R1—)(R2—)P—Y—P(—R3)(—R4)[/in-line-formulae] in which R1 to R4=unsubstituted aryl radicals or aryl radicals substituted with at least one radical exhibiting a positive resonance effect or a positive inductive effect, or unsubstituted or substituted cycloalkyl radicals, and Y=hydrocarbon group with a total of 2 to 20 carbon atoms, in which at least one of the carbon atoms carries only one or no hydrogen atom as substituent; except for the reaction of 4-bromo-3-difluoromethyl-1-methylpyrazole with 2-(3,4,5-trifluorophenyl)aniline and carbon monoxide to give N-[2-(3,4,5-trifluorophenyl)phenyl]-3-difluoromethyl-1-methylpyrazole-4-carboxamide.

Small molecule modifiers of MicroRNA miR-122 function for the treatment of hepatitis C Virus infection and hepatocellular carcinoma

MicroRNAs are a recently discovered new class of important endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation h