The Synthesis and Investigation of New Electroneutral Berberine Derivatives

Optimal synthesis conditions for NBF-modified 8,13-dihydroberberine derivatives

“…Scheme 3 shows two stages of the reaction for obtaining products 4a–11a , involving nucleophilic addition of acetophenone to form intermediates 4–11 and subsequent electrophilic substitution of hydrogen at the C-13 position with the pharmacophore to form 4a–11a . The first phase of the reaction was carried out using a methodology previously developed by us without modifications, 68 while the second stage of the process was the key focus of this study. It is worth noting that prior to our research, only 8-acetonyl, 8-alkyl, and 8-allyl-dihydroberberines (Scheme 1) were used for berberine modification.…”