Concise Synthesis of Versatile Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones

被引：6

作者：

Tran, Tuan P. ^{[1
]}

Fisher, Ethan L. ^{[1
]}

Wright, Ann S. ^{[1
]}

Yang, Jiao ^{[2
]}

机构：

[1] Pfizer Worldwide Res & Dev, Eastern Point Rd, Groton, CT 06340 USA

[2] WuXi AppTec, 288 Fute Zhong Rd, Shanghai 200131, Peoples R China

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2018年 / 22卷 / 02期

关键词：

N-AMINATION; PHOSPHODIESTERASE; HETEROCYCLES;

D O I：

10.1021/acs.oprd.7b00333

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The synthesis of a series of imidazo[S,1-f][1,2,4]triazin-4(3H)-ones was developed from starting imidazoles in three linear steps. The synthetic sequence began with an electrophilic amination and thus a rigorous campaign to identify safe reagent and reaction conditions was performed to ensure safety for preparation of these versatile intermediates on large scales. Functionalizations at the key positions on these substrates were exemplified to demonstrate ability to perform late-stage diversification for efficient SAR discovery.

引用

页码：166 / 172

页数：7

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