Synthesis of Mannose and Galactose Oligonucleotide Conjugates by Bi-click chemistry.

[摘要]：Glyco oligonucleotide conjugates, each exhibiting two mannose and two galactose residues, were efficiently synthesized by two successive 1,3-dipolar cycloaddn. (click chem.). Two phosphoramidite derivs. were used: one bearing a bromo-alkyl group as a precursor to azide functionalization and another bearing a propargyl group. After a first cycloaddn. with a mannosyl-azide deriv., the bromine atoms were substituted with NaN3 and a second click reaction was performed with a 1'-O-propargyl galactose, affording the hetero-glyco oligonucleotide conjugate.

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