437763-60-5

Upstream product

• 163704-72-1 4-nitro-2,6-diisopropyl aniline 
• 24544-04-5 2,6-diisopropylbenzenamine 
• 455288-51-4 4-amino-2,6-diisopropylaniline 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 620594-03-8 tert-butyl 4-nitrophenyl (2,6-diisopropyl-1,4-phenylene)biscarbamate 
• 437763-93-4 tert-butyl (4-{[({1-butyl-4-[3-(3-hydroxypropoxy)phenyl]-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl}-amino)carbonyl]amino}-3,5-diisopropylphenyl)carbamate 
• 476371-02-5 tert-butyl [4-({[(4-{3-[3-(benzyloxy)propoxy]phenyl}-1-butyl-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl)amino]carbonyl}amino)-3,5-diisopropylphenyl]carbamate 

Relevant academic research and scientific papers

Novel 1,4-diarylpiperidine-4-methylureas as anti-hyperlipidemic agents: Dual effectors on acyl-CoA:cholesterol O-acyltransferase and low-density lipoprotein receptor expression

A family of 1,4-diarylpiperidine-4-methylureas were designed and synthesized as novel dual effectors on ACAT and LDL receptor expression. We examined SAR of the synthesized compounds focusing on substitution at the three aromatic parts of the starting compound 1 and succeeded in identifying essential substituents for inhibition of ACAT and up-regulation of hepatic LDL receptor expression. Especially, we found that compound 12f, which can easily be prepared, has biological properties comparable to those of SMP-797, a promising ACAT inhibitor. In addition, the in vitro effects of 12f on lipid metabolism were substantially superior to those of a known ACAT inhibitor, Avasimibe.

Synthesis of SMP-797: A new potent ACAT inhibitor

A potent ACAT (acyl-CoA: cholesterol acyltransferase) inhibitor SMP-797 was effectively synthesized by the urea formation of 3-amino-4-aryl-1,8- naphthyridin-2(1H)-one and 4-amino-2,6-diisopropylamine. The synthesis of the former compound involved the Suzuki coupling reaction as a key step, and the latter was prepared by the 4-selective nitration of 2,6-diisopropylaniline using 2,3,5,6-tetrabromo-4-methyl-4-nitro-2,5-cyclohexadienone.