hfip辅助中继质子转移促进胺与乙烯基杂芳烃的共轭加成。

IF 3.3 3区化学 Q2 CHEMISTRY, MULTIDISCIPLINARY

Chemistry - An Asian Journal Pub Date : 2025-06-10 DOI:10.1002/asia.202500548

Arijit Mahana, Renuka Pradhan, Manas Kumar Sahu, Upakarasamy Lourderaj, Chidambaram Gunanathan

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引用次数: 0

摘要

以HFIP为最佳有效溶剂，研究了多种无环和环仲胺对2-乙烯基吡啶和乙烯基喹啉的Michael加成反应。利用该方案，成功合成了具有降压和抗眩晕特性的药物分子，环丙沙星在反应中是可调节的，为药物修饰提供了途径。DFT研究揭示了HFIP在溶剂辅助中继质子转移步骤中的作用，从而导致高产品收率。

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HFIP-Assisted Relay Proton Transfer Facilitates Conjugate Addition of Amines to Vinyl Heteroarenes.

The Michael addition reaction of diverse acyclic and cyclic secondary amines towards 2-vinyl pyridine and vinyl quinoline was explored, using HFIP as the optimal potent solvent. Using this protocol, drug molecules with hypotensive and antivertigo properties were successfully synthesized, and ciprofloxacin was amenable in the reaction offering a pathway for drug modification. DFT studies reveal the role of HFIP during the solvent-assisted relay proton transfer step, leading to high product yields.

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来源期刊

Chemistry - An Asian Journal 化学-化学综合

CiteScore

7.00

自引率

2.40%

发文量

535

审稿时长

1.3 months

期刊介绍： Chemistry—An Asian Journal is an international high-impact journal for chemistry in its broadest sense. The journal covers all aspects of chemistry from biochemistry through organic and inorganic chemistry to physical chemistry, including interdisciplinary topics. Chemistry—An Asian Journal publishes Full Papers, Communications, and Focus Reviews. A professional editorial team headed by Dr. Theresa Kueckmann and an Editorial Board (headed by Professor Susumu Kitagawa) ensure the highest quality of the peer-review process, the contents and the production of the journal. Chemistry—An Asian Journal is published on behalf of the Asian Chemical Editorial Society (ACES), an association of numerous Asian chemical societies, and supported by the Gesellschaft Deutscher Chemiker (GDCh, German Chemical Society), ChemPubSoc Europe, and the Federation of Asian Chemical Societies (FACS).