Synthesis and Reactivity of 18F-Labeled α,α-Difluoro-α-(aryloxy)acetic Acids

详细信息    查看全文

• 作者：Tanatorn Khotavivattana ; Samuel Calderwood ; Stefan Verhoog ; Lukas Pfeifer ; Sean Preshlock ; Neil Vasdev ; Thomas L. Collier ; Véronique Gouverneur
• 刊名：Organic Letters
• 出版年：2017
• 出版时间：February 3, 2017
• 年：2017
• 卷：19
• 期：3
• 页码：568-571
• 全文大小：376K
• ISSN：1523-7052

文摘

In this work, we describe the ¹⁸F-labeling of α,α-difluoro-α-(aryloxy)acetic acid derivatives and demonstrate that these building blocks are amenable to post-¹⁸F-fluorination functionalization. Protodecarboxylation offers a new entry to ¹⁸F-difluoromethoxyarene, and the value of this approach is further demonstrated with coupling processes leading to representative ¹⁸F-labeled TRPV1 inhibitors and TRPV1 antagonists.