845834-59-5

Upstream product

• 709-63-7 1-(4-trifluoromethylphenyl)ethanone 
• 6306-52-1 L-valine methylester hydrochloride 
• 1737-26-4 1-(4-trifluorophenyl)ethanol 
• 455-19-6 4-Trifluoromethylbenzaldehyde 

Downstream Products

• 845834-70-0 (2S)-2-{(2-chloroacetyl)[(1R)-1-(4-trifluoromethylphenyl)ethyl]amino}-3-methylbutyric acid methyl ester 
• 845834-61-9 (2S)-2-{(2-chloroacetyl)[(1S)-1-(4-trifluoromethylphenyl)ethyl]amino}-3-methylbutyric acid methyl ester 
• 845834-63-1 4-{3-isopropyl-2,5-dioxo-4-[1-(4-trifluoromethylphenyl)ethyl]piperazin-1-yl}piperidine-1-carboxylic acid tert-butyl ester 
• 845834-65-3 2-isopropyl-4-(piperidin-4-yl)-1-[1-(4-trifluoromethylphenyl)ethyl]piperazine 

Relevant academic research and scientific papers

An improved synthesis of piperazino-piperidine based CCR5 antagonists with flexible variation on pharmacophore sites

An improved and efficient synthetic route towards piperidino-piperazine based CCR5 antagonists was developed. The new approach was flexible for introducing various substituents in the pharmacophore sites via Grignard reagent addition and reductive amination. l-Amino acids were used as a chiral pool to introduce and then induce the desired stereochemistries, meanwhile rendering the variable substitution. The efficient construction of the piperazino-piperidine nucleus was achieved in a highly convergent manner with a key building block of N1-Boc-4-substituent-4-aminopiperidine, exhibiting significant advantages in terms of concise synthetic route and environmental-friendly reagents over the previously described stepwise synthesis, in which a modified Strecker reaction was involved with highly toxic reagents such as diethylaluminum cyanide.