58665-20-6

Upstream product

• 339363-11-0 3-Methyl-2-(methylpropylamino)-1-buten 
• 70-34-8 2,4-Dinitrofluorobenzene 
• 58665-17-1 (1,2-dimethyl-propylidene)-propyl-amine 
• 563-80-4 3-methyl-butan-2-one 
• 99-65-0 meta-dinitrobenzene 
• 1226526-98-2 1-(benzothiazole-2-sulfonyl)-1-(2,4-dinitro-phenyl)-3-methyl-butan-2-one 

Relevant academic research and scientific papers

A general and convenient method for the synthesis of 2,4-dinitrobenzyl ketones. Almost unlimited access to 2-substituted 6-nitroindoles from 2,4-dinitrotoluene and aldehydes

2,4-Dinitrotoluene reacts in the presence of catalytic amounts of DBU with aldehydes to form the corresponding alcohols in good yields (usually above 65%). The obtained alcohols can be readily oxidized to 2,4-dinitrobenzyl ketones, which were used for the synthesis of 6-nitroindoles with various substituents in the 2-position. Starting from non-racemic aldehydes, non-racemic 2-substituted 6-nitroindoles were obtained.

5-SULFAMOYL-2-HYDROXYBENZAMIDE DERIVATIVES

The invention is directed to substituted salicylamide derivatives. Specifically, the invention is directed to compounds according to Formula (I): wherein R, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, the treatment of HIV, autoimmune diseases, infections, atherosclerosis, and ischemia–reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Transition-metal-free formal sonogashira coupling and α-carbonyl arylation reactions

Transition-metal-free formal Sonogashira coupling and α-carbonyl arylation reactions have been developed. These transformations are based on the nucleophilic aromatic substitution (SNAr) of β-carbonyl sulfones to electron-deficient aryl fluorides, producing a key intermediate that, depending on the reaction conditions, gives the aromatic alkynes or α-aryl carbonyl compounds. The development of these reactions is presented and, based on investigations under basic and acidic conditions, mechanisms have been proposed. To develop the formal disclosed that expands the reaction concept. The scope of these reactions is demonstrated for the synthesis of Sonogashira and α-carbonyl arylated products from a range of electron-deficient aryl fluorides with a variety of functional groups and aryl-, heteroaryl-, alkyl-, and alkoxy-substituted sulfone nucleophiles. These transition-metal-free reactions complement the metal-catalyzed versions in terms of substitution patterns, simplicity, and reaction conditions.