Synthesis of a Key Intermediate towards the Preparation of Efavirenz Using n-Butyllithium
Tóm tắt
A key reaction in one of the routes to efavirenz, an essential drug used in the treatment of acquired immunodeficiency syndrome (AIDS), is the ortho-lithiation reaction of N-Boc-4-chloroaniline. For the first time, we demonstrate that the reaction may be conducted using n-BuLi and show that the reaction may be performed in a flow reactor with a significantly higher yield (70%) compared to batch (28%) when using n-BuLi for the ortho-metalation reaction at a temperature of −45 °C. In addition, it was shown that tetramethylethylenediamine (TMEDA) did not need to be added to the flow reaction, which simplified the purification procedure.
Từ khóa
#Chemistry/Food Science #general #Green Chemistry #Organic Chemistry #Inorganic Chemistry #Nanochemistry #Industrial Chemistry/Chemical EngineeringTài liệu tham khảo
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