Department of Nuclear Medicine, Seoul National University Hospital, Seongnam 13620, Republic of Korea.
Department of Transdisciplinary Studies, Graduate School of Convergence Science and Technology, Seoul National University, Seoul 08826, Republic of Korea.
Org Lett. 2020 Dec 18;22(24):9551-9555. doi: 10.1021/acs.orglett.0c03604. Epub 2020 Dec 3.
Methylated bis-triethylene glycolic crown-5-calix[4]arene (M-BTC5A) as a phase-transfer catalyst showed the best performance among other analogues and even conventional Kryptofix 222 in the nucleophilic aromatic F-fluorination of diaryliodonium tosylate precursors owing to (i) the efficient release of reactive "naked" [F]fluoride, (ii) the high stabilization of the precursor in the reaction, and, presumably, (iii) the ease of access between the precursor and the KF/M-BTC5A complex facilitated by π-π interactions. [F]Flumazenil was produced in high radiochemical yield using M-BTC5A.
甲氧基双三甘醇冠醚-5-杯[4]芳烃（M-BTC5A）作为相转移催化剂，在亲核芳香碘化砜盐前体的氟氟化反应中，表现出比其他类似物甚至传统的 Kryptofix 222 更好的性能，这是由于：（i）高效释放反应性的“裸露”[F]氟化物；（ii）在反应中高稳定的前体；以及（iii）可能通过π-π相互作用，使得前体和 KF/M-BTC5A 配合物之间易于接近。使用 M-BTC5A 可以高放射化学产率得到[F]氟马西尼。
