Synthesis of nucleoside libraries on solid support.: I.: N2,N6-disubstituted diaminopurine nucleosides

被引：7

作者：

Gunic, E ^{[1
]}

Amador, R ^{[1
]}

Rong, F ^{[1
]}

Abt, JW ^{[1
]}

An, HY ^{[1
]}

Hong, Z ^{[1
]}

Girardet, JL ^{[1
]}

机构：

[1] Ribapharm Inc, Costa Mesa, CA 92626 USA

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2004年 / 23卷 / 1-2期

关键词：

combinatorial library; nucleoside; purine;

D O I：

10.1081/NCN-120028342

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Starting with 2-iodo-6-chloro-9-(beta-D-ribofuranosyl)purine, a library of more than 1,300 N-2, N-6-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.

引用

页码：495 / 499

页数：5

共 8 条

[1] A NEW REAGENT FOR THE CLEAVAGE OF FULLY PROTECTED PEPTIDES SYNTHESIZED ON 2-CHLOROTRITYL CHLORIDE RESIN [J].