Solid-phase synthesis of N-9-substituted 2,8-diaminopurines

被引：11

作者：

Cole, Andrew G. ^{[1
]}

Metzger, Axel ^{[1
]}

Ahmed, Gulzar ^{[1
]}

Brescia, Marc-Raleigh ^{[1
]}

Chan, Ray J. ^{[1
]}

Wen, James ^{[1
]}

O'Brien, Linda ^{[1
]}

Qin, Lan-Ying ^{[1
]}

Henderson, Ian ^{[1
]}

机构：

[1] Pharmacopeia Drug Discovery Inc, Princeton, NJ 08543 USA

来源：

TETRAHEDRON LETTERS | 2006年 / 47卷 / 50期

关键词：

D O I：

10.1016/j.tetlet.2006.10.050

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A general and efficient solid-phase synthesis of N-9-substituted 2,8-diaminopurines from 5-nitrouracil is described. The key synthetic transformation employs a carbodiimide-mediated cyclization of a thiourea. Thiourea formation on solid phase is performed using both thermal and microwave reaction conditions. Regiospecific solution-phase synthesis of key building blocks allows the incorporation of desired substituents at N-9 of the purine nucleus. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：8897 / 8900

页数：4

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