66735-14-6

Upstream product

• 123-62-6 propionic acid anhydride 
• 1122-91-4 4-bromo-benzaldehyde 
• 110-89-4 piperidine 
• 516-05-2 methyl-propanedioic acid 
• 137-40-6 sodium proprionate 
• 106-40-1 4-bromo-aniline 
• 251320-24-8 2-[(4-bromo-phenyl)-hydroxy-methyl]-acrylic acid methyl ester 
• 1367876-28-5 [(Z)-3-(4-bromophenyl)-2-methoxycarbonyl-2-propenyl]triphenylphosphonium bromide 
• 103519-90-0 3-(4-bromophenyl)-2-methylacrylic acid ethyl ester 

Downstream Products

• 90766-74-8 4-Brom-β-brom-α-methyl-zimtsaeure 
• 1285505-56-7 N-[(E)-3-(4-furan-3-yl-phenyl)-2-methyl-acryloyl]-guanidine 
• 1285505-93-2 N-[(E)-3-(4-bromo-phenyl)-2-methyl-acryloyl]-guanidine 
• 66735-01-1 3-(4-bromophenyl)-2-methylpropanoic acid 
• 1040274-42-7 (S)-3-(4-Bromophenyl)-2-methylpropionic acid 
• 23773-30-0 (4-bromophenyl)-1-propyne 

Relevant academic research and scientific papers

Catalytic, enantioselective 1,2-difluorination of cinnamamides

The enantio- and diastereoselective synthesis of 1,2-difluorides via chiral aryl iodide-catalyzed difluorination of cinnamamides is reported. The method uses HF-pyridine as a fluoride source and mCPBA as a stoichiometric oxidant to turn over catalyst, and

Discovery of a novel inhibitor of nitric oxide production with potential therapeutic effect on acute inflammation

Inflammation as a host's excessive immune response to stimulation, is involved in the development of numerous diseases. To discover novel anti-inflammatory agents and based on our previous synthetic work on marine natural product Chrysamide B, it and a series of derivatives were synthesized and evaluated for their anti-inflammatory activity on inhibition of LPS-induced NO production. Then the preliminary structure–activity relationships were conducted. Among them, Chrysamide B is the most potent anti-inflammatory agent with low cytotoxicity and strong inhibition on the production of NO (IC50 = 0.010 μM) and the activity of iNOS (IC50 = 0.082 μM) in LPS-stimulated RAW 264.7 cells. Primary studies suggested that the mechanism of action may be that it interfered the formation of active dimeric iNOS but not affected transcription and translation. Furthermore, its good performance of anti-inflammatory effect on LPS-induced multiple inflammatory cytokines production, carrageenan-induced paw edema, and endotoxin-induced septic mice, was observed. We believe that these findings would provide an idea for the further modification and research of these analogs in the future.

Copper-Photocatalyzed Contra-Thermodynamic Isomerization of Polarized Alkenes

The contra-thermodynamic isomerization of α- and β-substituted cinnamate derivatives catalyzed by the Cu(OAc)2/rac-BINAP complex under blue light irradiation is reported. The use of an oxazolidinone template, which favored the complexation of the copper catalyst to the substrate, allowed the E → Z isomerization of the catalytically formed chromophore under simple and robust reaction conditions in good to excellent ratios. The mechanism of this process based on the transient formation of a chromophore was also studied.

Pd-Catalyzed α-Selective C-H Functionalization of Olefins: En Route to 4-Imino-β-Lactams

Pd-catalyzed α-olefinic C-H activation of simple α,β-unsaturated olefins has been developed. 4-imino-β-lactam derivatives were readily synthesized via activation of α-olefinic C-H bonds with excellent cis stereoselectivity. A wide range of heterocycles at the β-position are compatible with this reaction. The product of 4-imino-β-lactam derivatives can be readily converted to 2-aminoquinoline which exists extensively in pharmaceutical drugs and natural products.

Microwave-assisted synthesis of the (E)-α-methylalkenoate framework from multifunctionalized allylic phosphonium salts

A convenient and general microwave-assisted method for the synthesis of stereochemically defined α-methylalkenoic acids and esters from allylic phosphonium salts in a basic aqueous medium is described. A selective preparation of acids or esters was dependent on the base (NaOH or NaHCO 3) employed in the reaction and could be achieved with good to excellent yields under mild conditions in the absence of hydrides and reducing agents.

NOVEL ACYL GUANIDINE DERIVATIVES

The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.