Solid-phase synthesis of alpha-difluoro-beta-amino acids by a reformatsky reaction

摘要

Fluorine substitution is a highly effective approach for altering the chemical properties of compounds that affect the biological activity and pharmacological distribution of numerous,drugs,including anti-depressants,anti-inflammatory agents,anti-psychotics,steroids,antivirals and anesthetics.Given the importance of small molecule combinatorial libraries in the process of drug design,we decided to explore the synthesis of fluorinated compounds using solid-phase chemistry.The Reformatsky reaction with ethyl bromodifluoroacetate is commonly used for the incorporation of the -CF_2CO-group.