Synthesis of Nucleoside Libraries on Solid Support. I. N2,N6-Disubstituted Diaminopurine Nucleosides †.

Autor: Gunic, Esmir, Amador, Roberto, Rong, Frank, Abt, JeffreyW., An, Haoyun, Hong, Zhi, Girardet, Jean‐Luc
Předmět:
Zdroj: Nucleosides, Nucleotides & Nucleic Acids; Jan2004, Vol. 23 Issue 1/2, p495-499, 5p, 2 Diagrams
Abstrakt: Starting with 2-iodo-6-chloro-9-(β-D-ribofuranosyl) purine, a library of more than 1,300 N², N[sup6]-polysubstituted diaminopurine nucleosides was created. The starting material was condensed with a polystyrene monomethoxytrityl resin and a pool of primary and secondary amines was used to displace the 6-chloro atom with high regio-selectivity. The 2-iodo was subsequently displaced by various primary amines. Nucleosides were cleaved from the resin with hexafluoroisopropanol solutions. A majority of compounds reached a purity of more than 80% without the need for any type of purification. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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