Nakagawa Tomoki, Wada Yuki, Chan Bun, Baba Taichi, Hanaya Kengo, Koseki Yuta, Asano Ryuji, Aoki Katsuyuki, Usov Pavel M, Kawano Masaki
Department of Chemistry, School of Science, Institute of Science Tokyo, 2-12-1 Ookayama, Meguro-ku, Tokyo 152-8550, Japan.
TEKMOF Co., Ltd., INDEST, 3-3-6 Shibaura, Minato-ku, Tokyo 108-0023, Japan.
J Am Chem Soc. 2025 Aug 13;147(32):29013-29025. doi: 10.1021/jacs.5c07192. Epub 2025 Jul 31.
This study presents the development of a novel metal-organic framework (MOF) denoted as APF-80, suitable for the structural analysis of nucleophilic compounds that have traditionally been challenging to analyze using the crystalline sponge method. It was synthesized using a new mixed-substituent hexaazaphenalene ligand (344-TPHAP) featuring both 3-pyridyl and 4-pyridyl groups. This framework demonstrated remarkable stability toward nucleophilic molecules, which could be captured inside the pores through a synergistic combination of coordination and hydrogen-bonding interactions. APF-80 was successfully applied to determine the structures of 12 bioactive molecules, including naturally occurring alkaloids and pharmaceutical compounds. The host-guest interaction modes observed inside the resulting structures were classified into five distinct types. Binding energy calculations revealed that the guest site energies positively correlated with the crystallographic occupancies and the corresponding interaction types. This multimodal capture mechanism enabled the precise structural analysis of nucleophilic compounds under mild conditions, expanding the scope of molecules that can be analyzed by the crystalline sponge method.
本研究展示了一种新型金属有机框架(MOF)APF-80的开发,它适用于亲核化合物的结构分析,而传统上使用晶体海绵法对这些化合物进行分析具有挑战性。它是使用一种新型混合取代基六氮杂菲配体(344-TPHAP)合成的,该配体同时具有3-吡啶基和4-吡啶基。该框架对亲核分子表现出显著的稳定性,亲核分子可通过配位和氢键相互作用的协同组合被捕获在孔内。APF-80已成功应用于确定12种生物活性分子的结构,包括天然生物碱和药物化合物。在所得结构中观察到的主客体相互作用模式分为五种不同类型。结合能计算表明,客体位点能量与晶体占有率和相应的相互作用类型呈正相关。这种多模式捕获机制能够在温和条件下对亲核化合物进行精确的结构分析,扩大了可通过晶体海绵法分析的分子范围。