152906-79-1

Upstream product

• 74067-45-1 2-amino-5-chloro-α-(2'-chlorophenyl)benzyl alcohol 
• 630-19-3 pivalaldehyde 

Downstream Products

• 152906-99-5 ethyl 3-[N-[4-chloro-2-(2-chloro-α-hydroxybenzyl)phenyl]-N-neopentylcarbamoyl]acrylate 
• 1292849-65-0 methyl 4-[{4-chloro-2-[(2-chlorophenyl)(hydroxy)methyl]-phenyl}(2,2-dimethylpropyl)amino]-4-oxobutanoate 
• 1292849-71-8 1-{4-[{4-chloro-2-[(2-chlorophenyl)(hydroxy)methyl]-phenyl}(2,2-dimethylpropyl)amino]-4-oxobutanoyl}piperidine-4-carboxamide 
• 1292849-70-7 1-{4-[{4-chloro-2-[(2-chlorophenyl)(hydroxy)methyl]-phenyl}(2,2-dimethylpropyl)amino]-4-oxobutanoyl}-N-methylpiperidine-4-carboxamide 
• 1292849-69-4 1-{4-[{4-chloro-2-[(2-chlorophenyl)(hydroxy)methyl]-phenyl}(2,2-dimethylpropyl)amino]-4-oxobutanoyl}-N,N-dimethylpiperidine-4-carboxamide 
• 1292849-68-3 1-{4-[{4-chloro-2-[(2-chlorophenyl)(hydroxy)methyl]-phenyl}(2,2-dimethylpropyl)amino]-4-oxobutanoyl}piperidine-4-carboxylic acid 
• 1292849-67-2 ethyl 1-{4-[{4-chloro-2-[(2-chlorophenyl)(hydroxy)-methyl]phenyl}(2,2-dimethylpropyl)amino]-4-oxobutanoyl}-piperidine-4-carboxylate 
• 1292849-66-1 4-[{4-chloro-2-[(2-chlorophenyl)(hydroxy)methyl]-phenyl}(2,2-dimethylpropyl)amino]-4-oxobutanoic acid 
• 1292849-95-6 ethyl 1-(4-{[4-chloro-2-(2-chlorobenzyl)phenyl](2,2-dimethylpropyl)amino}-4-oxobutanoyl)piperidine-4-carboxylate 
• 1292849-94-5 4-chloro-2-(2-chlorobenzyl)-N-(2,2-dimethylpropyl)-aniline 
• 1292849-86-5 ethyl 1-{3-[{4-chloro-2-[(2-chlorophenyl)(hydroxy)-methyl]phenyl}(2,2-dimethylpropyl)amino]-3-oxopropanoyl}-piperidine-4-carboxylate 
• 1292849-85-4 ethyl 1-{5-[{4-chloro-2-[(2-chlorophenyl)(hydroxy)-methyl]phenyl}(2,2-dimethylpropyl)amino]-5-oxopentanoyl}-piperidine-4-carboxylate 
• 1292849-84-3 5-[{4-chloro-2-[(2-chlorophenyl)(hydroxy)methyl]phenyl}(2,2-dimethylpropyl)amino]-5-oxopentanoic acid 
• 1292849-82-1 ethyl (4-{4-[{4-chloro-2-[(2-chlorophenyl)(hydroxy)-methyl]phenyl}(2,2-dimethylpropyl)amino]-4-oxobutanoyl}-piperazin-1-yl)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.

Syntheses of fused heterocyclic compounds and their inhibitory activities for squalene synthase

A variety of fused heterocyclic compounds (2-11) were synthesized as a modification of the lead compound 1a and evaluated for their inhibition of squalene synthase. 4,1-Benzothiazepine derivative 2, 1,4-benzodiazepine derivative 6, 1,3-benzodiazepine derivative 7, 1-benzazepine derivative 9, and 4,1-benzoxazocine derivative 10 potently inhibited squalene synthase activity, whereas the 4,1-benzoxazepine derivatives 1 was the most potent inhibitor. 4,1-Benzothiazepine S-oxide derivative 4, 1,4-benzodiazepine derivative 5, 1,3,4-benzotriazepine derivative 8, and 1,2,3,4-tetrahydroquinoline derivative 11 were found to be weakly active. Comparison of the X-ray structures of these compounds (1a, 2, 4, 5, 7 and 10) suggests that orientation of the 5- (or 6)-phenyl group is important for activity. Copyright