Regioselective enzymatic acylation as a tool for producing solution-phase combinatorial libraries

摘要: Abstract A simple combinatorial strategy for sequential regioselective enzymatic acylation of multifunctional lead compounds has been developed and demonstrated using a polyhydroxylated flavonoid, bergenin, as model. The approach is based on the ability different enzymes to regioselectively acylate sites molecule without affecting other similar functional groups. In sharp contrast acylation, conventional chemical methods showed almost complete lack regioselectivity. was applied successfully produce solution phase library 167 distinct selectively acylated derivatives bergenin robotic workstation in 96-well plate format. General applicability automated biocatalysis discussed.