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

详细信息	查看全文 | 推荐本文 |

• 作者：Andrew G. Cole ; Axel Metzger ; Gulzar Ahmed ; Marc-Raleigh Brescia ; Ray J. Chan ; James Wen ; Linda O’ ; Brien ; Lan-Ying Qin ; Ian Henderson
• 刊名：Tetrahedron Letters
• 出版年：2006
• 期刊代码：109_00404039
• 类别：ch
• 出版时间：11 December 2006
• 卷：47
• 期：50
• 页码：8897-8900
• 文件大小：212 K

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.