一种用于新型嘌呤和核苷类似物的固相方法。

A solid-phase approach to novel purine and nucleoside analogs.

作者信息

Chang Junbiao, Dong Chunhong, Guo Xiaohe, Hu Weidong, Cheng Senxiang, Wang Qiang, Chen Rongfeng

机构信息

Henan Key Laboratory of Fine Chemicals, Zhengzhou 450002, PR China.

出版信息

Bioorg Med Chem. 2005 Aug 1;13(15):4760-6. doi: 10.1016/j.bmc.2005.05.007.

DOI:10.1016/j.bmc.2005.05.007

PMID:15946848

Abstract

This paper describes a method for the preparation of purine analogs using the solid-phase approach. Nucleoside bases were constructed on Merrifield resin by sequential displacement of purine dichloride with amines, and after detachment, the purine analogs were condensed with d,l-ribofuranoside compounds by the Vorbrüggen method. Thereof, l-ribofuranoside was prepared from l-arabinose via the selective oxidation-reduction procedure of the 2-OH group. Some compounds exhibited moderate activity against HIV-1 in PBM cells.

摘要

本文描述了一种使用固相方法制备嘌呤类似物的方法。通过用胺依次取代嘌呤二氯化物，在 Merrifield 树脂上构建核苷碱基，脱附后，通过 Vorbrüggen 方法将嘌呤类似物与 d，l-呋喃核糖苷化合物缩合。其中，l-呋喃核糖苷由 l-阿拉伯糖通过 2-OH 基团的选择性氧化还原程序制备。一些化合物在原代外周血单核细胞（PBM）细胞中对 HIV-1 表现出中等活性。