42498-44-2

Usage

Uses

Used in Pharmaceutical Industry:
BIPHENYL-3-CARBONYL CHLORIDE is used as a versatile intermediate for the synthesis of various pharmaceuticals. Its ability to form amides, esters, and other derivatives makes it an essential building block in the development of complex organic molecules for medicinal applications.
Used in Agrochemical Industry:
BIPHENYL-3-CARBONYL CHLORIDE is used as a key intermediate in the production of agrochemicals. Its reactivity with nucleophiles allows for the creation of various agrochemical compounds that can be used in crop protection and other agricultural applications.
Used in Specialty Chemicals Industry:
BIPHENYL-3-CARBONYL CHLORIDE is used as a crucial intermediate in the synthesis of specialty chemicals. Its strong acylating properties enable the formation of a wide range of chemical derivatives, contributing to the development of unique and specialized chemical products.
Used in Polymer and Resin Industry:
BIPHENYL-3-CARBONYL CHLORIDE is used as a component in the creation of polymers and resins. Its reactivity and ability to form various chemical derivatives make it a valuable building block in the development of polymers and resins with specific properties for various applications.
Used in Peptide Chemistry:
BIPHENYL-3-CARBONYL CHLORIDE is used as a coupling reagent in peptide chemistry. Its strong acylating properties facilitate the formation of peptide bonds, making it an important tool in the synthesis of peptides and other related compounds.
Safety Precautions:
Due to its hazardous nature, BIPHENYL-3-CARBONYL CHLORIDE should be handled with proper safety measures. Appropriate personal protective equipment, such as gloves, goggles, and lab coats, should be worn during its use. Additionally, it should be stored in a well-ventilated area, away from heat and open flames, to minimize the risk of accidents and exposure.

Upstream product

• 716-76-7 3-phenylbenzoic acid 
• 108-86-1 bromobenzene 
• 58313-23-8 3-iodobenzoic acid methyl ester 
• 24398-88-7 ethyl 3-bromobenzoate 
• 585-76-2 m-bromobenzoic acid 
• 16606-00-1 methyl 3-phenylbenzoate 
• 98-80-6 phenylboronic acid 
• 618-89-3 methyl 3-bromobenzoate 
• 2113-57-7 3-bromobiphenyl 
• 19926-50-2 biphenyl-3-carboxylic acid ethyl ester 

Downstream Products

• 153535-49-0 N-methoxy-N-methyl-[1,1'-biphenyl]-3-carboxamide 
• 938163-34-9 3-([1,1'-biphenyl]-3-yl)-3-oxopropanenitrile 
• 620937-51-1 N-benzyl-(1,1'-biphenyl)-3-carboxamide 
• 620937-65-7 N-cyclohexyl 3-phenylbenzamide 
• 1365682-49-0 2-(((2R)-3-(((2S)-3-(tert-butoxy)-1-methoxy-1-oxopropan-2-yl)amino)-2-((tert-butoxycarbonyl)amino)-3-oxopropyl)thio)ethyl [1,1'-biphenyl]-3-carboxylate 
• 873329-82-9 N-p-methylbenzylbiphenyl-3-carboxamide 
• 620937-44-2 N-propylbiphenyl-3-carboxamide 
• 620937-42-0 N-ethylbiphenyl-3-carboxamide 

Relevant academic research and scientific papers

Identification and Optimization of Novel Small-Molecule Cas9 Inhibitors by Cell-Based High-Throughput Screening

CRISPR/Cas9 has revolutionized several areas of life science; however, methods to control the Cas9 activity are needed for both scientific and therapeutic applications. Anti-CRISPR proteins are known to inhibit the CRISPR/Cas adaptive immunity; however, in vivo delivery of such proteins is problematic. Instead, small-molecule Cas9 inhibitors could serve as useful tools due to their permeable, proteolytically stable, and non-immunogenic nature. Here, we identified a small-molecule ligand with anti-CRISPR/Cas9 activity through a high-throughput screening utilizing an Escherichia coli selection system. Extensive structure-activity relationship studies, which involved a deconstruction-reconstruction strategy, resulted in a range of analogues with significant improvements in the inhibitory activity. Based on NMR and electrophoretic mobility shift assays, we propose that the inhibitory action of these compounds likely results from direct binding to apo-Cas9, preventing Cas9:gRNA complex formation. These molecules may find use as Cas9 modulators in various applications.

Remarkably Efficient Iridium Catalysts for Directed C(sp2)-H and C(sp3)-H Borylation of Diverse Classes of Substrates

Here we describe the discovery of a new class of C-H borylation catalysts and their use for regioselective C-H borylation of aromatic, heteroaromatic, and aliphatic systems. The new catalysts have Ir-C(thienyl) or Ir-C(furyl) anionic ligands instead of the diamine-type neutral chelating ligands used in the standard C-H borylation conditions. It is reported that the employment of these newly discovered catalysts show excellent reactivity and ortho-selectivity for diverse classes of aromatic substrates with high isolated yields. Moreover, the catalysts proved to be efficient for a wide number of aliphatic substrates for selective C(sp3)-H bond borylations. Heterocyclic molecules are selectively borylated using the inherently elevated reactivity of the C-H bonds. A number of late-stage C-H functionalization have been described using the same catalysts. Furthermore, we show that one of the catalysts could be used even in open air for the C(sp2)-H and C(sp3)-H borylations enabling the method more general. Preliminary mechanistic studies suggest that the active catalytic intermediate is the Ir(bis)boryl complex, and the attached ligand acts as bidentate ligand. Collectively, this study underlines the discovery of new class of C-H borylation catalysts that should find wide application in the context of C-H functionalization chemistry.

Design and synthesis of N-(3-sulfamoylphenyl)amides as Trypanosoma brucei leucyl-tRNA synthetase inhibitors

The protozoan parasite Trypanosoma brucei (T. brucei) causes human African trypanosomiasis (HAT), which is a fatal and neglected disease in the tropic areas, and new treatments are urgently needed. Leucyl-tRNA synthetase (LeuRS) is an attractive target for the development of antimicrobial agents. In this work, starting from the hit compound thiourea ZCL539, we designed and synthesized a series of amides as effective T. brucei LeuRS (TbLeuRS) synthetic site inhibitors. The most potent compounds 74 and 91 showed IC50 of 0.24 and 0.25 μM, which were about 700-fold more potent than the starting hit compound. The structure-activity relationship was also discussed. These compounds provided a new scaffold and lead compounds for further development of antitrypanosomal agents.

Ni-Catalyzed Aryl Sulfide Synthesis through an Aryl Exchange Reaction

A Ni-catalyzed aryl sulfide synthesis through an aryl exchange reaction between aryl sulfides and a variety of aryl electrophiles was developed. By using 2-pyridyl sulfide as a sulfide donor, this reaction achieved the synthesis of aryl sulfides without using odorous and toxic thiols. The use of a Ni/dcypt catalyst capable of cleaving and forming aryl-S bonds was important for the aryl exchange reaction between 2-pyridyl sulfides and aryl electrophiles, which include aromatic esters, arenol derivatives, and aryl halides. Mechanistic studies revealed that Ni/dcypt can simultaneously undergo oxidative additions of aryl sulfides and aromatic esters, followed by ligand exchange between the generated aryl-Ni-SR and aryl-Ni-OAr species to furnish aryl exchanged compounds.

Facile Synthesis of Alkylidene Phthalides by Rhodium-Catalyzed Domino C?H Acylation/Annulation of Benzamides with Aliphatic Carboxylic Acids

The Rh-catalyzed ortho-C(sp2)?H functionalization of 8-aminoquinoline-derived benzamides with aliphatic acyl fluorides generated in situ from the corresponding acids has been developed. This reaction initiated with 8-aminoquinoline-directed ortho-C(sp2)?H acylation, which was accompanied by subsequent intramolecular nucleophilic acyl substitution of amide group to produce alkylidene phthalides This approach exhibits high stereo-selectivity for Z-isomer products, and tolerates a variety of functional groups as well as aliphatic carboxylic acids with diverse structural scaffolds.

Cu-Catalyzed C-H Alkenylation of Benzoic Acid and Acrylic Acid Derivatives with Vinyl Boronates

An efficient Cu-catalyzed C-H alkenylation with acyclic and cyclic vinyl boronates was realized for the first time under mild conditions. The scope of the vinyl borons and the compatibility with functional groups including heterocycles are superior than Pd-catalyzed C-H coupling with vinyl borons, providing a reliable access to multisubstituted alkenes and dienes. Subsequent hydrogenation of the product from the internal vinyl borons will lead to installation of secondary alkyls.

PFKFB3 INHIBITORS AND THEIR USES

This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventiions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.

PROCESS FOR THE MANUFACTURE OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS

The present invention is directed to a process for the manufacture of a compound of formula (I) wherein Y is CHR7, CR7R8 or O, n is 0, 1 or 2, R1 and R2 are independently of each other selected from the group consisting of H, F, Cl, methyl and ethyl, and R3, R4, R5, R6, R7 and, R8 are independently of each other selected from H or C1-C6-alkyl. The compounds of formula (I) are 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors and can be used to reduce Cortisol levels in keratinocytes and to improve dermal collagen content in human skin after exposure to cortisone and UV.

Rhodium-Catalyzed Alkylation of C?H Bonds in Aromatic Amides with Non-activated 1-Alkenes: The Possible Generation of Carbene Intermediates from Alkenes

The alkylation of C?H bonds (hydroarylation) in aromatic amides with non-activated 1-alkenes using a rhodium catalyst and assisted by an 8-aminoquinoline directing group is reported. The addition of a carboxylic acid is crucial for the success of this reaction. The results of deuterium-labeling experiments indicate that one of deuterium atoms in the alkene is missing, suggesting that the reaction does not proceed through the commonly accepted mechanism for C?H alkylation reactions. Instead the reaction is proposed to proceed through a carbene mechanism. The carbene mechanism is also supported by preliminary DFT calculations.

Ligand-Promoted RhIII-Catalyzed Thiolation of Benzamides with a Broad Disulfide Scope

A ligand-promoted RhIII-catalyzed C(sp2)?H activation/thiolation of benzamides has been developed. Using bidentate mono-N-protected amino acid ligands led to the first example of RhIII-catalyzed aryl thiolation reactions directed by weakly coordinating directing amide groups. The reaction tolerates a broad range of amides and disulfide reagents.