C(1)-C(10)二羟基酸片段的C标记及其在Kulokekahilide-2 PET示踪剂合成中的应用

Chunguang Han, H. Doi, J. Kimura, Y. Nakao, Masaaki Suzuki
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引用次数: 3

摘要

以[11C]碘化甲酯和品那考烯基硼酸酯为原料,通过pd0介导的快速C-[11C]甲基化反应,成功合成了11C标记的库洛卡碱-2(1)的C1-C10部分结构。通过烯烃交叉复合反应制备有机硼中间体也是合成11c标记C1-C10二羟基酸片段1的关键步骤。
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11 C-Labeling of the C(1)-C(10) Dihydroxy Acid Moiety for the Study on the Synthesis of Kulokekahilide-2 PET Tracer
11C-labeled C1-C10 partial structure of kulokekahilide-2 (1) was successfully synthesized based on Pd0-mediated rapid C-[11C]methylation using [11C]methyl iodide and pinacol alkenylboronate. The preparation of organoboron intermediate via olefin cross-metathesis is also a crucial procedure for the synthesis of 11C-labeling C1-C10 dihy-droxy acid moiety of 1.
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