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

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journal contribution
posted on 06.11.2009, 00:00 by Insik Jeon, Karthik Iyer, Samuel J. Danishefsky
An improved synthesis of the hexasaccharide MBr1 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 a revised iodosulfonimidation/rearrangement.