Expedient Access to 2‐Benzazepines by Palladium‐Catalyzed C−H Activation: Identification of a Unique Hsp90 Inhibitor Scaffold,Chemistry - A European Journal

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Expedient Access to 2‐Benzazepines by Palladium‐Catalyzed C−H Activation: Identification of a Unique Hsp90 Inhibitor Scaffold
Chemistry - A European Journal ( IF 3.9 ) Pub Date : 2018-10-17 , DOI: 10.1002/chem.201804244
Matteo Virelli ₁ , Elisabetta Moroni ₂ , Giorgio Colombo _{1,

3} , Lorenzo Fiengo ₄ , Alessio Porta ₁ , Lutz Ackermann _{1,

5} , Giuseppe Zanoni ₁

Affiliation

Bioactive 2‐benzazepines were accessed in an atom‐ and step‐economical manner through a versatile palladium‐catalyzed C−H activation strategy. The C−H arylation required low catalyst loading and a mild base, which was reflected by a broad scope and high functional‐group tolerance. The benzotriazolodiazepinones were identified as new heat shock protein 90 (Hsp90) inhibiting lead compounds, with considerable potential for anti‐cancer applications.

中文翻译：

通过钯催化的CH活化方便地获得2-苯并ze庚因：鉴定独特的Hsp90抑制剂支架

生物活性的2-苯并ze庚因是通过通用的钯催化的CH活化方法以原子经济和分步经济的方式获得的。CH芳基化反应需要低的催化剂负载量和适度的碱，这反映在宽范围和高官能团耐受性上。苯并三唑并二氮杂吡啶酮被鉴定为新的抑制热激蛋白90（Hsp90）的先导化合物，在抗癌应用中具有相当大的潜力。

更新日期：2018-10-17

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