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Updated: Jun 9, 2025

Efficient Synthesis of Polyfunctionalized Benzenes in Water via Persulfate-promoted Benzannulation of α,β-Unsaturated Compounds and Alkynes
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Efficient Synthesis of Polyfunctionalized Benzenes in Water via Persulfate-promoted Benzannulation of α,β-Unsaturated Compounds and Alkynes

Published on: December 16, 2019

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增强基的芳香性可能会降低它们的代谢活性并降低它们的潜在细胞毒性:从对米里斯蒂辛和埃莱米的研究中吸取的教训

Guode Zhao1, Zixia Hu1, Jiannan Zheng1

  • 1Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, P. R. China.

Journal of medicinal chemistry
|October 23, 2024
PubMed
概括

由于由CYP3A4.4有效的代谢激活,素 (ELM) 比素 (MRS) 更有细胞毒性. 结构上的差异影响了与酶的相互作用,影响了反应性代谢物形成和药物开发潜力.

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Simple aryl halides do not react with nucleophiles. However, nucleophilic aromatic substitutions can be forced under certain conditions, such as high temperatures or strong bases. The mechanism of substitution under such conditions involves the highly unstable and reactive benzyne intermediate. Benzyne contains equivalent carbon centers at both ends of the triple bond, each of which is equally susceptible to nucleophilic attack. This 50–50 distribution of products is...
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All meta-directing substituents are deactivating groups. These substituents withdraw electrons from the aromatic ring, making the ring less reactive toward electrophilic substitution. For example, the nitration of nitrobenzene is 100,000 times slower than that of benzene because of the deactivating effect of the nitro group. The first step in an electrophilic aromatic substitution is the addition of an electrophile to form a resonance-stabilized carbocation. The energy diagrams for...
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