Synthesis of nucleoside libraries on solid support. I. N2,N6-disubstituted diaminopurine nucleosides |
| |
Authors: | Gunic Esmir Amador Roberto Rong Frank Abt Jeffrey W An Haoyun Hong Zhi Girardet Jean-Luc |
| |
Institution: | Ribapharm, Inc., Costa Mesa, California 92626, USA. |
| |
Abstract: | Starting with 2-iodo-6-chloro-9-(beta-D-ribofuranosyl)purine, a library of more than 1,300 N2,N6-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 regioselectivity. 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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|