436090-22-1

Upstream product

• 13296-94-1 2-bromo-4-nitroaniline 
• 614-76-6 N-acetyl-2-bromoaniline 
• 100-01-6 4-nitro-aniline 
• 57045-86-0 N-(2-bromo-4-nitro-phenyl)-acetamide 
• 7783-06-4 hydrogen sulfide 
• 7664-41-7 ammonia 

Downstream Products

• 488082-57-1 2-bromo-4-[3,3-diethyl-1-triazenyl]-N-acetylaniline 
• 488082-68-4 3-(2-acetylamino-5-trimethylsilanylethynyl-phenylethynyl)-5-trimethylsilanylethynyl-benzoic acid methyl ester 
• 488082-62-8 2-(2-acetylamino-5-trimethylsilanylethynyl-phenylethynyl)-4-trimethylsilanylethynyl-benzoic acid methyl ester 
• 488082-66-2 C₂₆H₃₃N₇O₃ 
• 488082-60-6 C₂₆H₃₃N₇O₃ 
• 488082-61-7 2-(2-acetylamino-5-iodo-phenylethynyl)-4-iodo-benzoic acid methyl ester 
• 488082-67-3 3-(2-acetylamino-5-iodo-phenylethynyl)-5-iodo-benzoic acid methyl ester 
• 488082-58-2 C₁₇H₂₆N₄OSi 
• 488082-64-0 C₁₄H₁₈N₄O 
• 488082-69-5 3-(2-acetylamino-5-ethynyl-phenylethynyl)-5-ethynyl-benzoic acid methyl ester 

Relevant academic research and scientific papers

Discovery of wtRET and V804MRET Inhibitors: From Hit to Lead

Oncogenic activation of RET kinase has been found in several neoplastic diseases, like medullary thyroid carcinoma, multiple endocrine neoplasia, papillary thyroid carcinoma, and non-small-cell lung cancer. Currently approved RET inhibitors were not originally designed to be RET inhibitors, and their potency against RET kinase has not been optimized. Hence, novel compounds able to inhibit both wild-type RET (wtRET) and its mutants (e.g., V804MRET) are needed. Herein we present the development and the preliminary evaluation of a new sub-micromolar wtRET/V804MRET inhibitor, N-(2-fluoro-5-trifluoromethylphenyl)-N′-{4′-[(2′′-benzamido)pyridin-4′′-ylamino]phenyl}urea (69), endowed with a 4-anilinopyridine structure, starting from our previously identified 4-anilinopyrimidine hit compound. Profiling against a panel of kinases indicated 69 as a multi cKIT/wtRET/V804MRET inhibitor.

Fe-Catalyzed Amination of (Hetero)Arenes with a Redox-Active Aminating Reagent under Mild Conditions

A novel and efficient Fe-catalyzed direct C?H amination (NH2) of arenes is reported using a new redox-active aminating reagent. The reaction is simple, and can be performed under air, mild, and redox-neutral conditions. This protocol has a broad substrate scope and could be used in the late-stage modification of bioactive compounds. Mechanistic studies demonstrate that a radical pathway could be involved in this transformation.

Hydrogen Bond-Stabilized Helix Formation of a m-Phenylene Ethynylene Oligomer

(Matrix Presented) Incorporation of a single hydrogen bonded β-turn mimic in the backbone of a m-phenylene ethynylene oligomer is shown to affect the thermodynamic properties of the folding reaction. Oligomers 1 and 2 both undergo solvophobic helix formation, but hydrogen bonded oligomer 1 was found to form a more stable helix with a higher tolerance to solvent denaturation than isomeric, non-hydrogen bonded oligomer 2.