201221-22-9

Upstream product

• 144261-18-7 4-chlorophenyl-2,2-dimethylpropyl amine 
• 29668-43-7 2,3-dihydro-benzo[1,4]dioxine-5-carbaldehyde 
• 1292850-59-9 N-{4-chloro-2-[2,3-dihydro-1,4-benzodioxin-5-yl-(hydroxy)methyl]phenyl}-2,2-dimethylpropanamide 
• 65854-91-3 N-(4-chlorophenyl)-2,2-dimethylpropionamide 
• 3282-30-2 pivaloyl chloride 
• 106-47-8 4-chloro-aniline 

Relevant academic research and scientific papers

Discovery of a new 2-aminobenzhydrol template for highly potent squalene synthase inhibitors

To obtain small and efficient squalene synthase inhibitors, a flexible 2-aminobenzhydrol open form structure was designed and showed potent inhibitory activity comparable to 4,1-benzoxazepin compounds. Further chemical modification led to the discovery of a novel template with a strong squalene synthase inhibitory activity, and its basic structure-activity relationship was revealed. The X-ray crystallographic data of compound 12 bound to the active site of squalene synthase provided an important insight into the binding mode of this alternative template that formed 11-membered ring conformations with an intramolecular hydrogen bond.

4,1-benzoxazepines or 4,1-benzothiazepines and their use as squalene synthetase inhibitors

This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, anti-Alzheimer's agents or anti-acne agents.