Dahl Kenneth, Lindberg Anton, Vasdev Neil, Schou Magnus
PET Science Centre, Precision Medicine and Biosamples, Oncology R&D, AstraZeneca, Karolinska Institutet, SE-17176 Stockholm, Sweden.
Department of Clinical Neuroscience, Centre for Psychiatry Research, Karolinska Institutet and Stockholm County Council, SE-17176 Stockholm, Sweden.
Pharmaceuticals (Basel). 2023 Jul 3;16(7):955. doi: 10.3390/ph16070955.
The Pd-Xantphos-mediated C-carbonylation protocol (also known as the "Xantphos- method"), due to its simplistic and convenient nature, has facilitated researchers in meeting a longstanding need for preparing C-carbonyl-labeled radiopharmaceuticals at ambient pressure for positron emission tomography (PET) imaging and drug discovery. This development could be viewed as a breakthrough in carbon-11 chemistry, as evidenced by the rapid global adoption of the method by the pharmaceutical industry and academic laboratories worldwide. The method has been fully automated for the good manufacturing practice (GMP)-compliant production of novel radiopharmaceuticals for human use, and it has been adapted for "in-loop" reactions and microwave technology; an impressive number of C-labeled compounds (>100) have been synthesized. Given the simplicity and efficiency of the method, as well as the abundance of carbonyl groups in bioactive drug molecules, we expect that this methodology will be even more widely adopted in future PET radiopharmaceutical research and drug development.
钯-双齿膦介导的碳羰基化反应方案（也称为“双齿膦法”），因其简单便捷的特性，助力研究人员满足了长期以来在环境压力下制备用于正电子发射断层扫描（PET）成像和药物研发的碳羰基标记放射性药物的需求。这一进展可被视为碳-11化学领域的一项突破，全球制药行业和学术实验室对该方法的迅速采用便是明证。该方法已实现全自动化，可用于符合药品生产质量管理规范（GMP）的新型供人类使用的放射性药物生产，并且已适用于“环内”反应和微波技术；已合成了数量可观的碳标记化合物（超过100种）。鉴于该方法的简单性和高效性，以及生物活性药物分子中羰基的丰富性，我们预计这种方法在未来的PET放射性药物研究和药物开发中将得到更广泛的应用。
