868066-28-8

Upstream product

• 655-32-3 2,2,2-trifluoro-1-(4-fluorophenyl)ethanone 
• 117009-97-9 benzyl 1,4-diazepane-1-carboxylate 

Downstream Products

• 1428556-50-6 benzyl 4-[4-(dimethylcarbamoyl)phenyl]-1,4-diazepane-1-carboxylate 
• 934744-14-6 benzyl 4-[4-(methylcarbamoyl)phenyl]-1,4-diazepane-1-carboxylate 
• 868066-34-6 4-(1,4-diazepan-1-yl)-N,N-dimethylbenzamide 
• 1428556-85-7 4-(1,4-diazepan-1-yl)-N-methylbenzamide 

Relevant academic research and scientific papers

Discovery and structure-activity relationship of thienopyridine derivatives as bone anabolic agents

A cell-based assay was performed for the discovery of novel bone anabolic agents. Alkaline phosphatase (ALPase) activity of ST2 cells was utilized as an indicator of osteoblastic differentiation, and thienopyridine derivative 1 was identified as a hit compound. 3-Aminothieno[2,3-b]pyridine-2-carboxamide was confirmed to be a necessary core structure for the enhancement of ALPase activity, and then optimization of the C4-substituent on the thienopyridine ring was carried out. Introduction of cyclic amino groups to the C4-position of the thienopyridine ring improved the activity. Especially, N-phenyl-homopiperazine derivatives were found to be strong enhancers of ALPase among this new series. Furthermore, 3-amino-4-(4-phenyl-1,4-diazepan-1-yl)thieno[2,3-b]pyridine-2- carboxamide (15k) was orally administered to ovariectomized (OVX) rats over 6 weeks for evaluating the effects on areal bone mineral density (aBMD), and statistically significant improvements in aBMD were observed from the dosage of 10 mg/kg/day.

THIENOPYRIDINE DERIVATIVES

The present invention provides a compound promoting osteogenesis. The present invention provides a compound having the following general formula (I) wherein R 1 is H or alkyl, R 2 is R a S-, R a O-, R a NH-, R a (R b )N- or cyclic amino, and R a and R b are alkyl which may be substituted, cycloalkyl which may be substituted, or the like, or a pharmacologically acceptable salt thereof.

A practical method for the preparation of 4-nitrogen-substituted benzoic acids

An efficient and practical method for the preparation of 4-nitrogen-substituted benzoic acids is described. Our method consists of the aromatic substitution of 2,2,2,4′-tetrafluoroacetophenone with amines, followed by haloform reaction to the benzoic acids. In this method, even though for the less nucleophilic 7-, 8-, and 9-membered amines 1 equiv. was used, corresponding benzoic acids were obtained in moderate to excellent yield. As the experimental procedure including purification is simple, this method is applicable to large-scale syntheses. Copyright