177410-73-0

Upstream product

• 3282-30-2 pivaloyl chloride 
• 152911-54-1 (+/-)-2-amino-5-chloro-α-(2,3-dimethoxyphenyl)benzyl alcohol 
• 106-47-8 4-chloro-aniline 
• 65854-91-3 N-(4-chlorophenyl)-2,2-dimethylpropionamide 
• 86-51-1 2,3-dimethyoxybenzaldehyde 

Downstream Products

• 152911-75-6 [5-chloro-2-(2,2-dimethylpropylamino)phenyl]-(2,3-dimethoxyphenyl)methanol 
• 177567-44-1 (E)-3-[{4-Chloro-2-[(S)-(2,3-dimethoxy-phenyl)-hydroxy-methyl]-phenyl}-(2,2-dimethyl-propyl)-carbamoyl]-acrylic acid ethyl ester 
• 177567-40-7 [(3R,5S)-7-Chloro-5-(2,3-dimethoxy-phenyl)-1-(2,2-dimethyl-propyl)-2-oxo-1,2,3,5-tetrahydro-benzo[e][1,4]oxazepin-3-yl]-acetic acid ethyl ester 
• 177410-76-3 (S)-(-)-5-chloro-α-(2,3-dimethoxyphenyl)-2-pivaloylaminobenzyl alcohol 
• 177410-77-4 (S)-[5-Chloro-2-(2,2-dimethyl-propylamino)-phenyl]-(2,3-dimethoxy-phenyl)-methanol 
• 171868-39-6 (3R,5S)-(-)-(3,5-trans)-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-1-neopentyl-2-oxo-4,1-benzoxazepine-3-acetic acid 
• 189059-58-3 (-)-2-amino-5-chloro-α-(2,3-dimethoxyphenyl)benzyl alcohol 
• 177410-67-2 (+/-)-5-chloro-α-(2,3-dimethoxyphenyl)-2-pivaloylaminobenzyl acetate 

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.

Microbial enantioselective ester hydrolysis for the preparation of optically active 4,1-benzoxazepine-3-acetic acid derivatives as squalene synthase inhibitors

Microbial enantioselective ester hydrolysis for the preparation of optically active (3R,5S)-(-)-5-phenyl-4,1-benzoxazepine-3-acetic acid derivatives as potent squalene synthase inhibitors was investigated. Pseudomonas diminuta and Pseudomonas taetrolens h