开发一种安全且可扩展的途径，以获得 tau PET 示踪剂前体。
Development of a safe and scalable route towards a tau PET tracer precursor.
机构信息
Pharma Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland.
Pharma Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland.
出版信息
Bioorg Med Chem. 2018 Feb 15;26(4):970-976. doi: 10.1016/j.bmc.2017.10.007. Epub 2017 Oct 12.
PMID:29074348
Abstract
A scalable 5-step synthesis of the diazacarbazole derivative 1 used as tau PET tracer precursor is reported. Key features of this synthesis include a Buchwald-Hartwig amination, a Pd catalyzed CH activation and a Suzuki-Miyaura cross-coupling.
摘要
报告了一种可扩展的 5 步合成哒嗪咔唑衍生物 1 的方法，该化合物可用作 tau PET 示踪剂前体。该合成的关键特点包括 Buchwald-Hartwig 胺化反应、Pd 催化的 CH 活化和 Suzuki-Miyaura 交叉偶联反应。
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