192379-53-6

Upstream product

• 7703-74-4 2,6-bis-(bromomethyl)pyridine 
• 1074-82-4 potassium phtalimide 

Downstream Products

• 192379-47-8 C₄₄H₅₄N₄O₉ 
• 192379-50-3 {2-[(6-Aminomethyl-pyridin-2-ylmethyl)-(2-nitro-benzenesulfonyl)-amino]-ethyl}-(3-hydroxy-propyl)-carbamic acid tert-butyl ester 
• 192379-49-0 {2-[[6-(1,3-Dioxo-1,3-dihydro-isoindol-2-ylmethyl)-pyridin-2-ylmethyl]-(2-nitro-benzenesulfonyl)-amino]-ethyl}-(3-hydroxy-propyl)-carbamic acid tert-butyl ester 
• 1431703-22-8 C₃₁H₂₄ClN₅O₄ 
• 1431701-25-5 C₂₈H₂₇N₇O₂ 
• 1431703-23-9 C₃₆H₂₉N₇O₄ 

Relevant academic research and scientific papers

Solution phase combinatorial chemistry. Synthesis of novel linear pyridinopolyamine libraries with potent antibacterial activity

Novel linear pyridinopolyamine derivatives 1-3, 7, and 8 have been synthesized as scaffolds for combinatorial drug discovery. The mono-t-Boc- and monotosyl-protected linear scaffolds 1 and 2 were obtained by a Schiff base type cyclization of 2,6-pyridinedicarboxaldehyde (24) with monoprotected triamines 22 and 23 using Ni2+ as a metal template, followed by reductive cleavage and decomplexation in a one-pot procedure. The unprotected linear scaffold 3 was obtained by treating 1 with TFA. Scaffold 1 was also synthesized from the orthogonally protected pyridinepolyamine 7 which was constructed from 2,6-bis(bromomethyl)pyridine (29) in four steps. Selective deprotection of the key intermediate 7 afforded 8, which was further selectively deprotected to give scaffold 1. A combinatorial chemistry strategy involving solution phase simultaneous addition of functionalities (SPSAF) is described. Thirteen high-purity tertiary amine libraries (9-21) (total 1638 compounds) were synthesized by the SPSAF and fix last methodologies from linear polyamine scaffolds 1 and 2. All libraries were examined by TLC, purified by chromategraphic techniques, and characterized by 1H NMR and ESI MS spectral data. A fix last methodology was utilized to minimize chemical reactions and perform SAR studies directly on libraries. Several first-round sublibraries of scaffold 1, containing 126 compounds each, exhibited potent antibacterial activity with MICs of 1-12 μM against Streptococcus pyogenes and Escherichia coli imp-.

ANTICANCER BENZOPYRAZINES VIA THE INHIBITION OF FGFR KINASES

The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.