A convenient synthesis of 5'-triantennary N-acetyl-galactosamine clusters based on nitromethanetrispropionic acid.
作者： Michael T. Migawa , Thazha P. Prakash , Guillermo Vasquez , W. Brad Wan , Jinghua Yu
DOI: 10.1016/J.BMCL.2016.03.070
关键词:
摘要: A convenient method for the synthesis of several triantennary GalNAc clusters based on a nitromethanetrispropionic acid core was developed. The synthetic approach involves pentafluorophenolic ester intermediates which can be used in one-pot, seven reaction procedure to quickly prepare variety conjugated ASOs. were 5'-end an antisense oligonucleotide and evaluated activity primary mouse hepatocytes where they showed ∼10-fold improvement activity.
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