Microwave-Assisted Rapid One-Pot Synthesis of Fused and Non-Fused Indoles and 5-[18 F]Fluoroindoles from Phenylazocarboxylates.

Microwave-Assisted Rapid One-Pot Synthesis of Fused and Non-Fused Indoles and 5-[18 F]Fluoroindoles from Phenylazocarboxylates.
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DOI:
10.1002/chem.201703890
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发表时间:
2017-11
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通讯作者:
Jasmin Krüll;A. Hubert;N. Nebel;O. Prante;M. Heinrich
Jasmin Krüll;A. Hubert;N. Nebel;O. Prante;M. Heinrich
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作者:
Jasmin Krüll;A. Hubert;N. Nebel;O. Prante;M. Heinrich

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取代吲哚可由苯偶氮甲酸酯通过一锅法快速合成,关键步骤为微波辅助的Fischer吲哚合成。考虑到苯偶氮甲酸酯可以预先通过温和的亲核芳香族取代反应进行修饰,包括引入[18F]氟化物,整个策略提供了一个有吸引力的新途径来获得5-[18F]氟吲哚。
Substituted indoles can be prepared from phenylazocarboxylates through a rapid one-pot sequence featuring a microwave-assisted Fischer indole synthesis as a key step. Considering that the phenylazocarboxylates may beforehand be modified by mild nucleophilic aromatic substitution, including the introduction of [18 F]fluoride, the overall strategy offers an attractive new access to 5-[18 F]fluoroindoles.