Divergent synthesis of novel 9-deazaxanthine derivatives via late-stage cross-coupling reactions

被引：3

作者：

Bartoccini, Francesca ^{[1
]}

Piersanti, Giovanni ^{[1
]}

Mor, Marco ^{[2
]}

Tarzia, Giorgio ^{[1
]}

Minetti, Patrizia ^{[3
]}

Cabri, Walter ^{[3
]}

机构：

[1] Univ Urbino, Dept Biomol Sci, I-61029 Urbino, Italy

[2] Univ Parma, Dipartimento Farmaceut, I-43124 Parma, Italy

[3] Sigma Tau Pharmaceut Co, Chem & Analyt Dev Dept, I-00040 Rome, Italy

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2012年 / 10卷 / 44期

关键词：

SOLID-PHASE SYNTHESIS; LINKED POLYSTYRENE BEARING; LONG-LIVED CATALYSTS; PHARMACOLOGICAL-PROPERTIES; ARYL CHLORIDES; POTENT; DESIGN; HETEROARYL; ANALOGS; METAL;

D O I：

10.1039/c2ob26516h

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A small library of 8-substituted 9-deazaxanthines has been prepared by late-stage diversification of an 8-bromo-9-deazaxanthine. By utilizing palladium-catalyzed cross-coupling reactions a single key precursor can be transformed into a variety of 8-substituted-9-deazaxanthine compounds. Three key 8-bromo-9-deazaxanthine intermediates were efficiently prepared from commercially available 6-chlorouracil in six steps.

引用

页码：8860 / 8867

页数：8

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