Concise Chemoenzymatic Total Synthesis of GE81112 B1 and Simplified Analogs Enable Elucidation of Its Key Pharmaco-phores

We report a chemoenzymatic total synthesis of GE81112 B1 that employs biocatalytic hydroxylation to prepare two of the key monomers of the target natural product. By pairing this strategy with traditional organic chemistry, we were able to synthesize GE81112 B1 in 11 steps. Following this strategy, six GE81112 analogs were synthesized, allowing for elucidation of its key pharmacophores.