855300-90-2

Upstream product

• 18197-26-7 sodium diformamide 
• 5000-66-8 2-chlorophenacyl bromide 
• 2142-68-9 1-(2-chlorophenyl)ethanone 

Downstream Products

• 855300-95-7 N-[2-(2-chloro-phenyl)-2-oxo-ethyl]-oxalamic acid ethyl ester 
• 855301-85-8 (Z)-2-Benzoylamino-3-[5-(2-chloro-phenyl)-thiazol-2-yl]-acrylic acid methyl ester 
• 855300-97-9 5-(2-chloro-phenyl)-thiazole-2-carbaldehyde 
• 855300-91-3 [5-(2-chloro-phenyl)-thiazol-2-yl]-methanol 
• 3811-25-4 clorprenaline 
• 23496-56-2 (+/-)-2-amino-1-(2-chlorophenyl)ethanol 
• 16442-79-8 2-amino-1-(2-chlorophenyl)ethan-1-one hydrochloride 

Relevant academic research and scientific papers

Preparation method of stable isotope-labeled clorprenaline

The invention relates to a preparation method of stable isotope-labeled clorprenaline. The preparation method comprises the following steps: with 2-bromo-2'-chloroacetophenone as an initial raw material, successively conducting improved Gabriel synthesis (wherein the initial raw material and an amination reagent sodium, namely diformyl amide are subjected to a nucleophilic substitution reaction), hydrolysis, reduction and reductive amination so as to synthesize the isotope-labeled clorprenaline . According to the preparation method disclosed by the invention, through a four-step conventional chemical reaction, process design is reasonable, raw material price is low, an experimental process is controllable, operation is simple and convenient, various required labeled compounds such as D-labeled, 13C-labeled or D/13C double-labeled compounds can be conveniently synthesized, the purity of the prepared target product is high and reaches 98% or above, total yield reaches 66% or above, the isotope abundance of the final product can reach 98% or above, the phenomenon of isotope abundance dilution is avoided, higher reproducibility and stability are achieved, and the obtained target compound can provide a standard reagent for accurately and quantitatively detecting trace residues of clorprenaline.

Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid

A novel series of nonnucleoside HCV NS5B polymerase inhibitors were prepared from (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid, a high throughput screening lead. SAR studies combined with structure based drug design focusing on the southern heterobiaryl region of the template led to the synthesis of several potent and orally bioavailable lead compounds. X-ray crystallography studies were also performed to understand the interaction of these inhibitors with HCV NS5B polymerase.