The glycosylation of opioid peptides has been shown to effectively increase blood-brain barrier (BBB) permeability and blood serum stability. This promising modification would allow delivery of neuropeptides into the CNS using peripheral administration. Previously, the large-scale production of glycosylated neuropeptides has been limited by the preparation of the glycosylated building blocks. The traditional approach to synthesizing glycosylated amino acids is a multi-step process that attains low to modest yields, making large-scale synthesis impractical. Using a Lewis acid as a promoter, however, microwave-assisted glycosylation of L-serine has been achieved with reasonable success. The reaction methodology is uncomplicated, and accommodates large-scale reactions while maintaining good yields. Thus far, glucoside, lactoside, and xyloside, serine-Fmoc compounds have been derived directly from their sugar peracetates. It was found that glycosylation was most effective using either FeCl3 or BF3*OEt2 in toluene, attaining a 55-65% percent yield that varied depending on the sugar used. However, additional Lewis acids continue to be explored.