A solid-phase approach towards the synthesis of PDE5 inhibitors

被引：13

作者：

Beer, D ^{[1
]}

Bhalay, G ^{[1
]}

Dunstan, A ^{[1
]}

Glen, A ^{[1
]}

Haberthuer, S ^{[1
]}

Moser, H ^{[1
]}

机构：

[1] Novartis Horsham Res Ctr, Horsham RH12 5AB, W Sussex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(02)00296-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

PDE5 inhibitors based upon the xanthine scaffold 8 have been expediently synthesized using a solid-phase route. Attachment of the xanthine scaffold 8 using the Rink chloride linker 4 and N-1 functionalization using Mitsunobu chemistry is described. A library of compounds was produced in multi-milligram quantities with excellent purities and acceptable yields. The compounds were tested for their PDE5 inhibitory activity. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1973 / 1976

页数：4

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