702641-01-8

Upstream product

• 1055901-15-9 2-(5-bromo-2-iodophenyl)acetonitrile 
• 1878-67-7 3-Bromophenylacetic acid 
• 20870-78-4 5-bromo-2-indolin-2-one 
• 878672-60-7 tert-butyl 2-(5-bromo-2-nitrophenyl)ethanoate 
• 878673-09-7 tert-butyl 2-(2-amino-3-methylphenyl)acetate 
• 586-78-7 para-nitrophenyl bromide 

Downstream Products

• 1055901-15-9 2-(5-bromo-2-iodophenyl)acetonitrile 

Relevant academic research and scientific papers

COMPOUNDS AND METHODS FOR MODULATING SPLICING

The present disclosure features compounds and related compositions that, inter alia, modulate nucleic acid splicing, e.g., splicing of a pre-mRNA, as well as methods of use thereof.

PROCESS FOR MAKING TETRACYCLIC HETEROCYCLE COMPOUNDS

The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that are useful as synthetic intermediates in the process of the invention.

Enantioselective Allylic C?H Oxidation of Terminal Olefins to Isochromans by Palladium(II)/Chiral Sulfoxide Catalysis

The enantioselective synthesis of isochroman motifs has been accomplished by palladium(II)-catalyzed allylic C?H oxidation from terminal olefin precursors. Critical to the success of this goal was the development and utilization of a novel chiral aryl sul

Ortho-stabilized 18F-azido click agents and their application in PET imaging with single-stranded DNA aptamers

Azido 18F-arenes are important and versatile building blocks for the radiolabeling of biomolecules via Huisgen cycloaddition ("click chemistry") for positron emission tomography (PET). However, routine access to such clickable agents is challenged by inefficient and/or poorly defined multistep radiochemical approaches. A high-yielding direct radiofluorination for azido 18F-arenes was achieved through the development of an ortho-oxygen-stabilized iodonium derivative (OID). This OID strategy addresses an unmet need for a reliable azido 18F-arene clickable agent for bioconjugation reactions. A ssDNA aptamer was radiolabeled with this agent and visualized in a xenograft mouse model of human colon cancer by PET, which demonstrates that this OID approach is a convenient and highly efficient way of labeling and tracking biomolecules. Markedly apt: A high-yielding direct radiofluorination strategy via ortho-oxygen-substituted iodonium derivatives is described. A ssDNA aptamer (sgc8), labelled with the resulting 18F azido agent through click chemistry, was used for PET imaging and provides the first example for the noninvasive in vivo PET imaging of protein tyrosine kinase 7 (PTK-7).

Efficient synthesis of heterocyle-fused β-naphthylamines via intramolecular addition to a cyano group initiated by nucleopalladation of alkynes

A palladium(II)-catalyzed efficient synthesis of heterocycle-fused-naphthylamines was accomplished via nucleophilic addition of a carbon-palladium bond to the intramolecular cyano group initiated by nucleopalladation (oxypalladation or aminopalladation) o

COMPOUNDS FOR TREATING NEURODEGENERATIVE DISEASES

The invention provides novel tricyclic compounds of Formula (I) that inhibit B-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.

Expedient drug synthesis and diversification via ortho-C-H iodination using recyclable PdI2 as the precatalyst

(Figure Presented) Pd(II)-catalyzed ortho-C-H iodination reactions of phenylacetic acid substrates have been achieved using recyclable PdI2 as the precatalyst. This class of substrates is incompatible with the classic amide formation/ortho-lithiation/iodination sequence. The power of this new technology is demonstrated by facile drug functionalization and drastically shortened syntheses of the drugs diclofenac and lumiracoxib.

SUBSTITUTED AMINO PHENYLACETIC ACIDS, DERIVATIVES THEREOF, THEIR PREPARATION AND THEIR USE AS CYCLOOXYGENASE 2 (COX-2) INHIBITORS

Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C3-C8)cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted β-naphthyl, bicyclic heterocyclic aryl, (C3-C6)cycloalkylmonocyclic carbocyclic aryl, or (C5 or C6)cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof, and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.