1334126-75-8

Upstream product

• 2393-23-9 4-methoxy-benzylamine 
• 84249-14-9 2-amino-4-bromopyridine 
• 56651-60-6 4-methoxybenzyl isocyanate 

Downstream Products

• 1334127-91-1 1-(4-methoxybenzyl)-3-(4-(thiophen-2-yl)pyridin-2-yl)urea 
• 1334127-88-6 1-(4-methoxybenzyl)-3-(4-(2-methoxyphenyl)pyridin-2-yl)urea 
• 1334127-94-4 1-(2-fluoro-3,4'-bipyridin-2'-yl)-3-(4-methoxybenzyl)urea 

Relevant academic research and scientific papers

Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: An fast and atom efficient access to 1-aryl-3-benzylureas

The glycogen synthase kinase 3 (GSK-3) is implicated in multiple cellular processes and has been linked to the pathogenesis of Alzheimer's disease (AD). In the course of our research topic we synthesized a library of potent GSK-3 inhibitors. We utilized the urea scaffold present in the potent and highly selective GSK-3 inhibitor AR-A014418 (AstraZeneca). This moiety suits both (a) a convergent approach utilizing readily accessible building blocks and (b) a divergent approach based on a microwave heating assisted Suzuki coupling. We established a chromatography-free purification method to generate products with sufficient purity for the biological assays. The structure-activity relationship of the library provided the rationale for the synthesis of the benzothiazolylurea 66 (IC50 = 140 nM) and the pyridylurea 62 (IC 50 = 98 nM), which displayed two to threefold enhanced activity versus the reference compound 18 (AR-A014418: IC50 = 330 nM) in our assays.