118380-03-3

Upstream product

• 39552-81-3 methyl p-aminophenylacetate 
• 108-24-7 acetic anhydride 
• 67-56-1 methanol 
• 1197-55-3 4-aminophenylacetic acid 
• 106-40-1 4-bromo-aniline 
• 103-88-8 4-bromoacetanilide 
• 292638-85-8 acrylic acid methyl ester 
• 622-50-4 4-Acetamido-1-iodobenzene 
• 540-37-4 p-aminoiodobenzene 
• 18699-02-0 4-acetamidophenylacetic acid 
• 64-19-7 acetic acid 

Downstream Products

• 303050-39-7 methyl 2-(4-acetamido-3-nitrophenyl)acetate 
• 1613057-26-3 methyl (p-acetylaminophenyl)(trifluoromethylthio)acetate 
• 1026940-70-4 2-(4-Amino-3-nitro-phenyl)-N-((R)-5-methoxy-1,2,3,4-tetrahydro-naphthalen-1-ylmethyl)-N-methyl-acetamide 
• 1026426-43-6 4-{2-[((R)-5-Methoxy-1,2,3,4-tetrahydro-naphthalen-1-ylmethyl)-methyl-amino]-ethyl}-benzene-1,2-diamine 
• 116435-82-6 2-(4-amino-3-nitrophenyl)acetic acid 

Relevant academic research and scientific papers

An antibody transesterase derived from reactive immunization that utilizes a wide variety of alcohol substrates

A monoclonal antibody obtained from reactive immunization catalyzes transesterifications of alcohol substrates with both broad and unusual specificity.

Z-Selective Fluoroalkenylation of (Hetero)Aromatic Systems by Iodonium Reagents in Palladium-Catalyzed Directed C?H Activation

The direct and catalytic incorporation of fluorine containing molecular motifs into organic compounds resulting high-value added chemicals represents a rapidly evolving part of synthetic methodologies, thus this area is in the focus of pharmaceutical and agrochemical research. Herein we report a stereoselective procedure for direct fluorovinylation of aromatic and heteroaromatic scaffolds. This methodology development has been realized by palladium-catalyzed ortho C?H activation reaction of aniline derivatives featuring the regioselectivity via directing groups such as secondary of tertiary amides, ureas or ketones. The application of non-symmetrical aryl(fluoroalkenyl)-iodonium salts as fluoroalkenylating agents allowed mild reaction conditions in general for this transformation. The scope and limitations have been thoroughly investigated and the feasibility has been demonstrated by more than 50 examples.

Green Esterification of Carboxylic Acids Promoted by tert-Butyl Nitrite

In this work, the green esterification of carboxylic acids promoted by tert-butyl nitrite has been well developed. This transformation is compatible with a broad range of substrates and exhibits excellent functional group tolerance. Various drugs and substituted amino acids are applicable to this reaction under near neutral conditions, with good to excellent yields.

HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR

Disclosed are heterocyclic compounds as inhibitors of FGFR-4 represented by formula (I). Also disclosed is a pharmaceutical composition that includes an inhibitor of FGFR-4. The compounds maybe used to treat diseases mediated with abnormality of FGFR-4 and /or FGF19, such as hepatocellular carcinoma and other forms of cancer.

Mild and efficient palladium-catalyzed direct trifluoroethylation of aromatic systems by C-H activation

The introduction of trifluoroalkyl groups into aromatic molecules is an important transformation in the field of organic and medicinal chemistry. However, the direct installation of fluoroalkyl groups onto aromatic molecules still represents a challenging and highly demanding synthetic task. Herein, a simple trifluoroethylation process that relies on the palladium-catalyzed C-H activation of aromatic compounds is described. With the utilization of a highly active trifluoroethyl(mesityl)iodonium salt, the developed catalytic method enables the first highly efficient and selective trifluoroethylation of aromatic compounds. The robust catalytic procedure provides the desired products in up to 95 % yield at 25 °C in 1.5 to 3 hours and tolerates a broad range of functional groups. The utilization of hypervalent reagents opens new synthetic possibilities for direct alkylations and fluoroalkylations in the field of transition-metal-catalyzed C-H activation.

A one-pot process for palladium catalyzed direct C-H acylation of anilines in water using a removable ortho directing group

A new mild, practical method for the synthesis of aminobenzophenone derivatives through a three step one-pot reaction sequence involving acylation of anilines, palladium catalyzed cross-dehydrogenative coupling of the formed anilides and the hydrolytic cleavage is reported. The full reaction sequence was performed under aqueous conditions.

Ti/Ni-mediated inter- and intramolecular conjugate addition of aryl and alkenyl halides and triflates

In this work, we show that the unique combination of a nickel catalyst and Cp2TiCl allows the direct conjugate addition of aryl and alkenyl iodides, bromides, and to a lesser extent, chlorides and triflates to α,β-unsaturated carbonyls at room temperature, without requiring the previous formation of an organometallic nucleophile. The reaction proceeds inter- and intramolecularly with good functional group compatibility, which is key for the development of free protecting group methodologies. Carbo- and heterocycles of five- and six-membered rings are obtained in good yields. Moreover, some insights about the mechanism involved have been obtained from cyclic voltammetry, UV-vis, and HRTEM measurements.

Structure-activity studies for a novel series of N-(arylethyl)-N- (1,2,3,4-tetrahydronaphthalen-1-ylmethyl)-N-methylamines possessing dual 5- HT uptake inhibiting and α2-antagonistic activities

In search of an α2-antagonist/5-HT uptake inhibitor as a potential new class of antidepressant with a more rapid onset of action, compound 3 was prepared and observed to possess high affinity for the α2-receptor (K(i) = 6.71 nM) and