With a suitable enzyme in hand, we explored optimization of the reaction conditions (see SI). Working at these low enzyme concentrations we were able to lower NADPH loading from 25 mol% to 1 mol%, using GDH/glucose as an efficient cofactor recycling system. Increasing methanol concentration (25%) was found to be detrimental to enzyme activity. Despite this, an increase in substrate loading as a suspension was tolerated up to 10 mM, albeit at a lower rate of conversion. The transformation could be pushed to completion by further increasing the enzyme loading and reaction time (1.0 mol%, 30 min). Initial efforts to scale the reaction revealed that on a 20 mL scale at [7a] = 2 mM, 50% conversion could be achieved (1.0 mol%, 2 h). The product could be isolated (36%) in >95% purity. Work is currently ongoing to further improve this conversion by optimizing reaction conditions towards process applications.