331779-03-4

Upstream product

• 5459-35-8 2-bromo-acrylic acid ethyl ester 
• 589-87-7 1,4-bromoiodobenzene 
• 106-37-6 1.4-dibromobenzene 
• 18620-02-5 (4-bromophenyl)magnesium bromide 
• 20201-26-7 ethyl 4-bromophenylglyoxylate 
• 50-00-0 formaldehyd 
• 14062-25-0 Ethyl 4-bromophenylacetate 

Downstream Products

• 1264519-70-1 (S)-3-tert-butyl 1-(phenanthren-9-yl) 1-(4-bromophenyl)cyclopent-3-ene-1,3-dicarboxylate 
• 1264518-99-1 phenanthren-9-yl 2-(4-chlorophenyl)acrylate 
• 28131-17-1 2-(4-bromophenyl)acrylic acid 
• 1629188-73-3 (2Z,4E)-ethyl 2-(4-bromophenyl)-5-(4-chlorophenyl)penta-2,4-dienoate 

Relevant academic research and scientific papers

Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells

In this study, a series of thieno [2,3-d]pyrimidine derivatives were designed, synthesized and evaluated as novel AKT1 inhibitors. In vitro antitumor assay results showed that compounds 9d-g and 9i potently suppressed the enzymatic activities of AKT1 and

Iodonium Ylides as Carbene Precursors in Rh(III)-Catalyzed C-H Activation

The rhodium(III)-catalyzed coupling of C-H substrates with iodonium ylides has been realized for the efficient synthesis of diverse cyclic skeletons, where the iodonium ylides have been identified as efficient and outstanding carbene precursors. The reaction systems are applicable to both sp2 and sp3 C-H substrates under mild and redox-neutral conditions. The catalyst loading can be as low as 0.5 mol % in a gram-scale reaction. Representative products exhibit cytotoxicity toward human cancer cells at nanomolar levels.

Stereoselective synthesis of Z-vinylsilanes via palladium-catalyzed direct intermolecular silylation of C(sp2)-H bonds

An efficient and convenient palladium-catalyzed direct intermolecular silylation of C(sp2)-H bonds by using disilanes as the silicon source with the assistance of a readily removable bidentate directing group is reported. This strategy provided a regio- and stereoselective protocol for exclusive synthesis of Z-vinylsilanes with reasonable to excellent yields and good functional group compatibility. Silylation of the isolated palladacycle intermediate revealed the Z-stereoselective pathway. Moreover, the practicality and effectiveness of this method were illustrated by a gram-scale experiment and further functionalization of the silylation product.

Switchable C-H Functionalization of N-Tosyl Acrylamides with Acryloylsilanes

A controllable Rh-catalyzed protocol to access alkylation and alkenylation-annulation of N-tosyl acrylamide with acryloyl silane is reported. In contrast to the directing group or catalyst-dependent divergent sp2 C-H alkylation/alkenylation, the intrinsic property of acryloylsilane allows the switchable reaction manifold, thereby affording either alkylation or annulation products with slight modification of the reaction conditions.

Stereo- and chemoselective cross-coupling between two electron-deficient acrylates: An efficient route to (Z, E)-muconate derivatives

A Ru-catalyzed direct oxidative cross-coupling reaction of acrylates was developed. It offers a straightforward and atom-economical protocol for the synthesis of functionalized (Z,E)-muconate derivatives in moderate to good yields with good stereo- and chemoselectivities. The conjugated muconates bearing differentiable terminal functionality can be selectively transformed into versatile synthetic intermediates widely used in organic synthesis.

TYK2 INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

NOVEL ORTHO-AMINOANILIDES FOR THE TREATMENT OF CANCER

The present invention is directed to a compound of formula I, and processes for the manufacture of said compounds as well as medicaments containing said compound. The compounds according to this invention show anti-proliferative and differentiation-induci

Isoxazoline derivative and a process for the preparation thereof

The present invention provides to an isoxazoline derivative of formula (I), the pharmaceutically acceptable salts, esters and stereochemically isomeric forms thereof, and the use of the derivative in inhibiting the activity of caspases. The present invent

Facile synthesis of ethyl 2-arylpropenoates by cross-coupling reaction using electrogenerated highly reactive zinc

Highly reactive zinc metal was prepared by electrolysis of a DMF solution containing naphthalene and a supporting electrolyte in a one-compartment cell fitted with a platinum cathode and a zinc anode. This reactive zinc was used for efficient transformation of ethyl 2-bromoacrylate into the corresponding organozinc compound, which was reacted with various aryl iodides or bromides in the presence of 5 mol% Pd(P(o-Tol)3)2Cl2 to give the corresponding cross-coupling products in high yields. These cross-coupling reactions were successfully applied to a synthesis of the precursor of naproxen and cicloprofen, non-steroidal anti-inflammatory agent.

Facile synthesis of 2-arylpropenoic acid esters by cross-coupling using electrogenerated highly reactive zinc and a palladium catalyst

Highly reactive zinc metal was prepared by electrolysis of a DMF solution containing naphthalene and a supporting electrolyte in a one-compartment cell fitted with a platinum cathode and a zinc anode. The reaction of this reactive zinc with ethyl 2-bromoacrylate at -20 °C and the following cross-coupling reaction with aryl iodides in the presence of 5 mol% Pd(P(o-Tol)3)2Cl2 at 70 °C gave the corresponding ethyl 2-arylpropenoates in almost quantitative yields.