Two-step tandem synthesis of sugar-containing pyrimidine derivatives catalyzed by Lipozyme® TL IM in continuous-flow microreactors

Abstract

A novel series of sugar-containing pyrimidine derivatives have been synthesized via an effective and convenient two-step tandem synthesis in continuous-flow microreactors with excellent regioselectivity. Using continuous-flow microreactors to assemble two-step reactions into one unit can effectively avoid separating and purifying intermediates. Moreover, this method allows the optimization of reaction parameters for each unit individually. The salient features of this method include a reduction in the use of DMSO and mild reaction conditions (30–40 °C). Under the optimum reaction conditions, we can obtain the desired yield (34.8–69.1%) in a shorter time (40 min) than the shaking condition (48 h).