In this contribution,
we report the chemoenzymatic preparation
of a key building block for the active pharmaceutical ingredient rosuvastatin,
one of the “top 5 blockbuster drugs” with a worldwide
market value of 6.25 billion USD in 2012, via a seven-step synthesis
without isolation of intermediates and with incorporation of two highly
efficient biotransformations. This chemoenzymatic process reaches
excellent space-time yields by using high substrate concentrations
(several hundred grams per liter), emphasizing the potential of biocatalysis
for industrial processes related to pharmaceutical drug synthesis
and the compatibility of enzyme chemistry with classical organic synthesis