353246-06-7

Upstream product

• 290325-99-4 2-nitro-[N-(2{2[(2-nitrophenyl)sulfonylamino]ethylamino})ethyl]benzenesulfonamide 
• 1694-92-4 2-Nitrobenzenesulfonyl chloride 
• 7703-74-4 2,6-bis-(bromomethyl)pyridine 
• 353246-03-4 4-((tert-butoxycarbonyl)methyl)-1,7-bis(2-nitrophenylsulfonyl)-1,4,7-triazaheptane 

Relevant academic research and scientific papers

MACROCYLIC LIGANDS WITH PICOLINATE GROUP(S), COMPLEXES THEREOF AND ALSO MEDICAL USES THEREOF

The present invention relates to compounds, ligands, and/or complexes that are useful in medical imaging and/or in therapy, especially in cancer treatment. The present invention also relates to a pharmaceutical composition comprising said compounds, ligands, and/or complexes that are useful for medical imaging, targeting, and/or treatment of cancers. The present invention also relates to a process for preparing these compounds, ligands, and/or complexes.

Regioselective synthesis of N-functionalized 12-membered azapyridinomacrocycles bearing trialkylcarboxylic acid side chains

Selective protection of primary amine moieties of diethylenetriamine by 2-nitrophenylsulfonyl chloride followed by alkylation of the central N atom generates functionalized disulfonamide building blocks. When reacted with 2,6-bis(bromomethyl)pyridine following the Richman-Atkins methodology, such compounds yield the corresponding pyridine-containing azamacrocycles. Smooth removal of the N-sulfonyl groups provides versatile azamacrocyclic intermediates with transannular secondary amine functions. Subsequent N-alkylation regioselectively leads to tri N-functionalized 12-membered azapyridinomacrocycles bearing a sequence of N-acetate and N-propionate side chains.