1222709-23-0

Upstream product

• 50-00-0 formaldehyd 
• 94127-05-6 ethyl 3-[(aminocarbonyl)diazenyl]but-2-enoate 
• 62-53-3 aniline 
• 104953-98-2 C₇H₁₀N₂O₄C₂H₄ 
• 609-15-4 ethyl 2-chloro-3-oxo-butyrate 
• 51605-32-4 ethyl 4⁽⁵⁾-methylimidazole-5⁽⁴⁾-carboxylate 
• 98-80-6 phenylboronic acid 
• 51605-32-4 Ethyl 5-Methyl-4-imidazolecarboxylate 

Relevant academic research and scientific papers

CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF

Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.

Development of Highly Affine and Selective Fluorinated Cannabinoid Type 2 Receptor Ligands

Cannabinoid type 2 receptors (CB2 receptors) are involved in various pathological processes, and the visualization of their in vivo availability with positron emission tomography (PET) is of high interest. The study focuses on the introduction of fluorine into the structure of the highly affine and selective CB2 receptor ligand N-(adamantan-1-yl)-5-ethyl-2-methyl-1-phenyl-1H-imidazole-4-carboxamide (5). A novel series of compounds was developed by modifying (i) the adamantane-3-position, (ii) the imidazole-N-phenyl ring, and (iii) the imidazole-2-position, and the impact on the CB2 binding affinity and selectivity toward cannabinoid type 1 receptors (CB1) was evaluated. This study identified compound 15 as one of the most potent (Ki(CB2) = 0.29 nM) and selective (CB1/CB2 > 10000) CB2receptor ligands discovered so far, eligible for the development of an18F-labeled PET radiotracer.

One-pot synthesis of imidazole-4-carboxylates by microwave-assisted 1,5-electrocyclization of azavinyl azomethine ylides

Diversely functionalized imidazole-4-carboxylates were synthesized by microwave-assisted 1,5-eletrocyclization of 1,2diaza-l,3-diene-derived azavinyl azomethine ylides. 1,2-Diaza-1,3-dienes were treated with primary aliphatic or aromatic amines and subjected to microwave irradiation in the presence of aldehydes. 3-Alkyl- and 3-arylimidazole-4-carboxylates were prepared in good yields through a one-pot multicomponent procedure. Modulation of the substituents at C-2, N-3, and C-5 was possible, and 2-unsubstituted imidazoles were obtained when paraformaldehyde was used.