Abstract

Fused-ring systems containing heterocycles are attractive templates for drug discovery. Biologically active 6-5-5+6 fused-ring systems that possess heterocycles are available, but these require a relatively large number of synthetic steps for preparation. Therefore, pyrazolofuropyrazine was designed as a 6-5-5+6 ring system template that incorporates ready accessibility for drug discovery. Pyrazolofuropyrazines were successfully constructed in only a few steps via one-pot S_NAr reaction/intramolecular C–H direct arylation. As a drug candidate, pyrazolofuropyrazine has earned a favorable LogP, although significant biological activity has yet to be established; the ready accessibility of pyrazolofuropyrazine template, however, offers an opportunity for the rapid development of promising new drug candidates.

Fused-ring systems containing heterocycles are attractive templates for drug discovery. Biologically active 6-5-5+6 fused-ring systems that possess heterocycles are available, but these require a relatively large number of synthetic steps for preparation. Therefore, pyrazolofuropyrazine was designed as a 6-5-5+6 ring system template that incorporates ready accessibility for drug discovery. Pyrazolofuropyrazines were successfully constructed in only a few steps via one-pot S_NAr reaction/intramolecular C–H direct arylation. As a drug candidate, pyrazolofuropyrazine has earned a favorable LogP, although significant biological activity has yet to be established; the ready accessibility of pyrazolofuropyrazine template, however, offers an opportunity for the rapid development of promising new drug candidates.

中文翻译：

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一锅SNAr反应和分子内直接CH芳基化反应合成吡唑并呋喃并吡嗪

摘要

含有杂环的稠环系统是用于药物发现的有吸引力的模板。具有杂环的具有生物活性的6-5-5 + 6稠环系统是可用的，但是这些系统需要相对大量的合成步骤来制备。因此，吡唑并呋喃并吡嗪被设计为6-5-5 + 6环系统模板，并结合了药物发现的现成可及性。吡唑并呋喃并吡嗪通过一锅S _N Ar反应/分子内C–H直接芳基化仅需几个步骤即可成功构建。作为候选药物，吡唑并呋喃并吡嗪获得了良好的LogP，尽管尚未确立显着的生物学活性。吡唑并呋喃并吡嗪模板的现成可及性为快速开发有前途的新候选药物提供了机会。

含有杂环的稠环系统是用于药物发现的有吸引力的模板。具有杂环的具有生物活性的6-5-5 + 6稠环系统是可用的，但是这些系统需要相对大量的合成步骤来制备。因此，吡唑并呋喃并吡嗪被设计为6-5-5 + 6环系统模板，并结合了药物发现的现成可及性。吡唑并呋喃并吡嗪通过一锅S _N Ar反应/分子内C–H直接芳基化仅需几个步骤即可成功构建。作为候选药物，吡唑并呋喃并吡嗪获得了良好的LogP，尽管尚未确立显着的生物学活性。吡唑并呋喃并吡嗪模板的现成可及性为快速开发有前途的新候选药物提供了机会。