444915-84-8

Upstream product

• 3609-53-8 methyl 4-acetylbenzoate 
• 38078-09-0 diethylamino-sulfur trifluoride 

Downstream Products

• 55805-25-9 [4-(1,1-difluoroethyl)phenyl]methanol 
• 55805-22-6 4-(1,1-difluoroethyl)benzaldehyde 
• 945610-07-1 2-fluoro-2-(4-(methoxycarbonyl)phenyl)propanoic acid 

Relevant academic research and scientific papers

Visible-light photoredox-catalyzed selective carboxylation of C(sp3)?F bonds with CO2

It is highly attractive and challenging to utilize carbon dioxide (CO2), because of its inertness, as a nontoxic and sustainable C1 source in the synthesis of valuable compounds. Here, we report a novel selective carboxylation of C(sp3)?F bonds with CO2 via visible-light photoredox catalysis. A variety of mono-, di-, and trifluoroalkylarenes as well as α,α-difluorocarboxylic esters and amides undergo such reactions to give important aryl acetic acids and α-fluorocarboxylic acids, including several drugs and analogs, under mild conditions. Notably, mechanistic studies and DFT calculations demonstrate the dual role of CO2 as an electron carrier and electrophile during this transformation. The fluorinated substrates would undergo single-electron reduction by electron-rich CO2 radical anions, which are generated in situ from CO2 via sequential hydride-transfer reduction and hydrogen-atom-transfer processes. We anticipate our finding to be a starting point for more challenging CO2 utilization with inert substrates, including lignin and other biomass.

Gem-difluoro ethyl substitutional diphenylethene and diphenylethane derivative as well as preparation method and application thereof

The invention discloses gem-difluoro ethyl substitutional diphenylethene and diphenylethene diphenylethane derivatives as well as a preparation method and application thereof. A 4' bit of a B aromatic ring of diphenylethane/diphenylethene is subjected to chemical structure modification through gem-difluoro ethyl, and meanwhile, a 2' bit is modified into nitro or an amino group and other substituent groups; the gem-difluoro ethyl substitutional diphenylethene and diphenylethane derivative has relatively high antitumor activity in vitro, and the antitumor activity of a trans-form is better than the antitumor activity of a cis-form; with the introduction of fluorine atoms, not only is the physical property of the compound changed, but also the antitumor activity in vitro is improved at the same time, and the derivative has a relatively good inhibiting effect on multiple tumor cells.

Metal-free18F-labeling of aryl-CF2H via nucleophilic radiofluorination and oxidative C-H activation

A metal-free and selective method to form [18F]aryl-CF2H through nucleophilic radiofluorination of benzyl (pseudo)halides and oxidative C-H activation of benzylic C-H bonds has been developed. The method is operationally simple and tolerates a variety of electron-neutral/deficient arenes and heteroarenes.

BICYCLIC AZAHETEROCYCLIC COMPOUNDS AS NR2B NMDA RECEPTOR ANTAGONISTS

Disclosed are chemical entities of Formula (I): wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).

PYRROLO AND PYRAZOLOPYRIMIDINES AS UBIQUITIN-SPECIFIC PROTEASE 7 INHIBITORS

The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where m, n, X1, X2, R1-R5, R5′ and R6 are described herein.

FLUOROISOQUINOLINE SUBSTITUTED THIAZOLE COMPOUNDS AND METHODS OF USE

The invention relates to thiazole compounds of Formula (I) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.