2065-04-5

Upstream product

• 99-03-6 1-(3-aminophenyl)ethanone 
• 1939-99-7 benzenesulfonyl chloride 
• 2417-42-7 1-[3-[N-(methylsulfonyl)amino]phenyl]ethanone 

Downstream Products

• 1477503-64-2 N-(3-(6-(trifluoromethyl)imidazo[1,2-a]pyridin-2-yl)phenyl)methanesulfonamide 
• 193761-73-8 (+/-)-N-[5-(2-bromo-1-hydroxyethyl)-2-benzyloxyphenyl]-N,N-dimethylsulfamide 
• 79406-64-7 N-[3-(2-Amino-1-hydroxy-ethyl)-phenyl]-methanesulfonamide 
• 79889-61-5 N-(3-Benzo[d]imidazo[2,1-b]thiazol-2-yl-phenyl)-methanesulfonamide 
• 801150-73-2 N-[3-(2-Amino-acetyl)-phenyl]-methanesulfonamide 

Relevant academic research and scientific papers

Synthesis and biological evaluation of glucagon-like peptide-1 receptor agonists

In this study, a series of fused-heterocyclic derivatives were systematically designed and synthesized using an efficient route, and evaluated in terms of GLP-1R agonist activity. We employed short synthetic steps and reactions that are tolerant of the presence of various functional groups and suitable for parallel operations to enable the rapid generation of libraries of diverse and structurally complex small molecules. Of the compounds synthesized, 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a] pyridin-2-yl)phenyl methanesulfonate (8e) was the most potent agonist with an EC50 of 7.89 μM, and thus is the compound with the greatest potential for application. These findings represent a valuable starting point for the design and discovery of small-molecule GLP-1R agonists that can be administered orally.

METHOD FOR THE PREPARATION OF TRICYCLIC AMINO ALCOHOL DERIVATIVES THROUGH AZIDES

The present invention is directed to processes for the preparation of a tricyclic amino-alcohol derivative useful for treating and preventing diabetes, obesity, hyperlipidemia and the like, which compound is represented by the formula (1): wherein R1 represents a lower alkyl group or a benzyl group; *1 represents an asymmetric carbon atom; R2 represents a hydrogen atom, a halogen atom or a hydroxyl group; and A represents one of the following groups: wherein X represents NH, O or S; R5 represents a hydrogen atom, a hydroxyl group, an amino group or an acetylamino group; and *2 represents an asymmetric carbon atom when R5 is not a hydrogen atom. The processes of the present invention proceed via azide derivatives and are convenient, practical preparing processes with low cost which comprise a small number of steps with good industrial work efficiency.

Tricyclic compounds and drug compositions containing the same

Compounds having a β-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2 NR4 R4', or nitro; R6 represents hydrogen or lower alkyl; and X represents nitrogen, R9 represents hydrogen, one of R7 and R8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.