1086601-87-7

Upstream product

• 75-16-1 methylmagnesium bromide 
• 84459-33-6 2-bromo-4-chlorobenzaldehyde 
• 74-83-9 methyl bromide 
• 825-40-1 2-bromo-p-chloroacetophenone 

Downstream Products

• 1086599-76-9 1-(2-bromo-4-chlorophenyl)ethanamine 
• 1415130-74-3 ethyl 3-(5-(5-chloro-2-(1-((4'-fluoro-[1,1'-biphenyl]-4-yl)amino)ethyl)phenyl)picolinamido)propanoate 
• 1414931-70-6 Ethyl 5'-chloro-2'-(1-((4'-chloro-[1,1'-biphenyl]-4-yl)amino)ethyl)-[1,1'-biphenyl]-4-carboxylate 
• 825-40-1 2-bromo-p-chloroacetophenone 
• 1415128-92-5 3-(5-(5-chloro-2-(1-((4'-fluoro-[1,1'-biphenyl]-4-yl)amino)ethyl)phenyl)picolinamido)propanoic acid 
• 1414931-69-3 N-(1-(2-bromo-4-chlorophenyl)ethyl)-4'-chloro-[1,1'-biphenyl]-4-amine 
• 1414931-82-0 5'-chloro-2'-(1-((4'-chloro-[1,1'-biphenyl]-4-yl)amino)ethyl)-[1,1'-biphenyl]-4-carboxylic acid 
• 1414931-39-7 3-(5'-chloro-2'-(1-((4'-chloro-[1,1'-biphenyl]-4-yl)amino)ethyl)-[1,1'-biphenyl]-4-ylcarboxamido)propanoic acid 
• 1414931-71-7 ethyl 3-(5'-chloro-2'-(1-((4'-chloro-[1,1'-biphenyl]-4-yl)amino)ethyl)-[1,1'-biphenyl]-4-ylcarboxamido)propanoate 

Relevant academic research and scientific papers

α-Oxocarboxylic Acids as Three-Carbon Insertion Units for Palladium-Catalyzed Decarboxylative Cascade Synthesis of Diverse Fused Heteropolycycles

A novel palladium-catalyzed decarboxylative cascade cyclization for the assembly of diverse fused heteropolycycles by employing α-oxocarboxylic acids as three-carbon insertion units is reported. This protocol enables the synthesis of isoquinolinedione- and indolo[2,1-a]isoquinolinone-fused benzocycloheptanones in moderate to good yields by the use of different aryl iodides, including alkene-tethered 2-iodobenzamides and 2-(2-iodophenyl)-1H-indoles. Notably, the approach achieves simultaneous construction of both six- and seven-membered rings via sequential intramolecular carbopalladation, C-H activation, and decarboxylation.

Atmosphere-Controlled Palladium-Catalyzed Divergent Decarboxylative Cyclization of 2-Iodobiphenyls and α-Oxocarboxylic Acids

A novel palladium-catalyzed divergent decarboxylative cyclization of 2-iodobiphenyls and α-oxocarboxylic acids utilizing the atmosphere as a controlled switch is reported. Under the protection of a nitrogen atmosphere, tribenzotropones are synthesized by a [4 + 3] decarboxylative cyclization. Employing a palladium/O2 system enables a [4 + 2] decarboxylative cyclization to assemble triphenylenes. Notably, preliminary mechanistic studies indicate that the formation of triphenylenes involves a double decarboxylation.

The intramolecular reaction of acetophenoneN-tosylhydrazone and vinyl: Br?nsted acid-promoted cationic cyclization toward polysubstituted indenes

In the presence of TsNHNH2, a Br?nsted acid-promoted intramolecular cyclization ofo-(1-arylvinyl) acetophenone derivatives was developed, leading to polysubstituted indenes with complexity and diversity in moderate to excellent yields. In sharp contrast with either the radical or carbene involved cyclization of aldehydicN-tosylhydrazone with vinyl, a cationic cyclization pathway was involved, whereN-tosylhydrazone served as an electrophile and alkylation reagent during this transformation.

Asymmetric Synthesis and Application of Chiral Spirosilabiindanes

Reported here is the development of a class of chiral spirosilabiindane scaffolds by Rh-catalyzed asymmetric double hydrosilation, for the first time. Enantiopure SPSiOL (spirosilabiindane diol), a new type of chiral building block for the preparation of various chiral ligands and catalysts, was readily prepared on greater than 10 gram scale using this protocol. The potential of this new spirosilabiindane scaffold in asymmetric catalysis was preliminarily demonstrated by development of the corresponding monodentate phosphoramidite ligands (SPSiPhos), which were used in both a Rh-catalyzed hydrogenation and a Pd-catalyzed intramolecular carboamination.

PdII-Catalyzed Oxidative Tandem aza-Wacker/Heck Cyclization for the Construction of Fused 5,6-Bicyclic N,O-Heterocycles

A PdII-catalyzed oxidative tandem cyclization was developed for the construction of fused 5,6-bicyclic N, O-heterocycles. This reaction was enabled by the combined use of a 3-methylpyridine ligand and pentafluorobenzoic acid additive. A range of heterocyclic products with different substituents could be prepared in moderate to good yields via this methodology. Several transformations, including a scaled-up preparation of product 2 a, were also carried out showing the good applicability of our methodology.

Preparation of isoindolinones via a palladium-catalyzed diamination

A Pd(II)-catalyzed cyclization using oxidative olefin diamination was developed for the preparation of isoindolinones from ortho-olefinic N-methoxybenzamides. Using the optimized reaction conditions, the desired products were obtained in up to 90% yield using NFSI as the oxidant. This reaction provides an efficient and direct access to isoindolinones with amine functionality, an important drug skeleton.

Palladium-Catalyzed Aerobic Aminooxygenation of Alkenes for Preparation of Isoindolinones

A palladium-catalyzed intramolecular isoindolinone-forming aminooxygenation of alkenes with 1 atm of oxygen as oxidant is reported. A variety of functionalized alkenes and carboxylic acids can be used, and high yields were observed. Preliminary mechanistic studies revealed that the aminooxygenation products were formed through the oxidation of a C-PdII species using a strong oxidant, peroxide, which is generated in situ from a Pd(OAc)2/bpy/O2/HOAc catalytic system.

BIPHENYL DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS

The present invention is directed to biphenyl derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.

PICOLINAMIDO-PROPANOIC ACID DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS

The present invention is directed to picolanmido-propanoic acid derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.