摘要：2025年8月28日，北京——日本庆应义塾大学大松亨介教授做客康龙化成第五十八期“合成与药物化学前沿”名师线上讲座，所作报告的主题为“两性离子的光催化反应活性”。报告重点内容包括：1）稳定的酰胺类两性离子催化剂的设计与合成；2）酰胺类两性离子催化剂在光催化合成

转自：康龙化成

康龙化成举办第五十八期“合成与药物化学前沿”名师线上讲座

2025年8月28日，北京——日本庆应义塾大学大松亨介教授做客康龙化成第五十八期“合成与药物化学前沿”名师线上讲座，所作报告的主题为“两性离子的光催化反应活性”。报告重点内容包括：1）稳定的酰胺类两性离子催化剂的设计与合成；2）酰胺类两性离子催化剂在光催化合成反应中的应用；3）以膦叶立德为底物，开发生成新型卡拜活性中间体的新方法。

首先，大松亨介教授阐述了两性离子在光催化反应中具有良好的应用潜力，但由于其稳定性和反应活性难以兼顾，此前的化学合成研究中较少受到关注。为此，大松教授课题组以传统的氧中心自由基催化剂为参照，设计并成功合成了可转化为氮中心自由基的三氮唑两性离子催化剂。该类催化剂结构多样，可通过微调改变其电子效应和位阻效应。

随后，大松教授展示了其课题组早期开发的酰胺类两性离子催化剂在光敏剂协同下，实现了未活化C(sp³)–C(sp²)偶联反应。与传统方法需使用大过量烷烃底物不同，该方法仅需当量烷烃参与，显著提高了原子经济性。此外，近期开发的吖啶-酰胺类两性离子光催化剂在脱氢及脱羧C(sp³)–C(sp²)偶联反应中也表现出优异活性。这些方法学的建立降低了低活性底物间C–C键构建的难度。

最后，大松教授介绍了其课题组对膦叶立德类化合物的研究，开发出一种不同于传统路径的卡拜活性中间体合成策略，并实现了该中间体参与的三组分环加成反应。该方法能以优异产率制备多种环己烯及环戊烯类产物，为卡拜中间体的合成与应用提供了新思路。

会后，在问答环节中，大松亨介教授与听众进行了热烈讨论。

Frontiers in Synthetic and Medicinal Chemistry

--The 58th Pharmaron Virtual Lecture

Beijing, August 28, 2025—Professor Kohsuke Ohmatsu from Keio University, Japan, presented at the 58th "Frontiers in Synthetic and Medicinal Chemistry" Pharmaron virtual lecture series. The title of his presentation was "Photocatalytic Reactivity of Zwitterions." The report focused on the following key aspects: 1) The design and synthesis of stable amide-based zwitterionic catalysts; 2) The application of amide-based zwitterionic catalysts in photocatalytic synthetic reactions; 3) The development of a novel method for generating new carbyne active intermediates using phosphonium ylide substrates.

First, Professor Kohsuke Ohmatsu elaborated on the significant potential of zwitterions in photocatalytic reactions. However, due to the challenge of balancing stability and reactivity, they received limited attention in previous chemical synthesis research. To address this issue, Professor Kohsuke Ohmatsu's research group designed and successfully synthesized triazole zwitterionic catalysts that can convert into nitrogen-centered radicals, using traditional oxygen-centered radical catalysts as a reference. These catalysts exhibit structural diversity, allowing for fine-tuning of their electronic and steric properties.

Professor Kohsuke Ohmatsu presented his group's earlier work on amide-based zwitterionic catalysts, which, in combination with a photosensitizer, enabled unactivated C(sp³)–C(sp²) coupling reactions. Unlike conventional methods that require a large excess of alkane substrates, this approach utilizes only stoichiometric amounts of alkanes, thereby significantly improving atom economy. Additionally, recently developed acridine-amide-based zwitterionic photocatalysts demonstrated excellent activity in both dehydrogenative and decarboxylative C(sp³)–C(sp²) coupling reactions. These methodological advances have lowered the barrier for C–C bond formation between low-reactivity substrates.

Finally, Professor Kohsuke Ohmatsu shared his group's research on phosphonium ylide compounds, leading to the development of a novel strategy for synthesizing carbyne active intermediates via a non-traditional pathway. This was followed by the achievement of a three-component cycloaddition reaction involving these carbyne intermediates. The method enables the synthesis of various cyclohexene and cyclopentene derivatives in high yields, providing new insights into the synthesis and application of carbyne intermediates.

After the presentation, Professor Kohsuke Ohmatsu engaged in a lively discussion with the audience during the Q&A session.

来源：新浪财经