A Practical Total Synthesis of Globo-H for Use in Anticancer Vaccines

An improved synthesis of the hexasaccharide M Br 1 antigen (globo-H) is reported. Enhanced efficiency in the synthesis was necessary for the scale-up production of globo-H, in order to advance globo-H-based anticancer vaccines to clinical trials. The key features of the improved synthesis include preactivation-based glycosylations and it revised iodosulfonimidation/rearrangement.