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Updated: Jul 17, 2025

A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones
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A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones

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合成和评估具有读透诱导活性的新型三衍生物

Shota Kawai1, Shunsuke Takashima1, Masafumi Ando1

  • 1Drug Discovery Research Department, Kyoto Pharmaceutical Industries, Ltd.

Chemical & pharmaceutical bulletin
|September 4, 2023
PubMed
概括

新型三基衍生物KY-516有效诱导无意义突变的读透. 这种化合物通过恢复缺陷的酶生物合成,显示出作为Hurler综合征治疗剂的显著潜力.

关键词:
这就是阿塔勒伦 (Ataluren) 的意思.粘膜多糖症 I-hurler 的情况没有意义的突变突变.过早终止的代码子阅读通过通过.

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All ortho–para directors, excluding halogens, are activating groups. These groups donate electrons to the ring, making the ring carbons electron-rich. Consequently, the reactivity of the aromatic ring towards electrophilic substitution increases. For instance, the nitration of anisole is about 10,000 times faster than the nitration of benzene. The electron-donating effect of the methoxy group in anisole activates the ortho and para positions on the ring and stabilizes the corresponding...
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