Loreau Olivier, Marlière Philippe
CEA - iBiTecS, Service de Chimie Bioorganique et de Marquage, Gif sur Yvette, France.
J Labelled Comp Radiopharm. 2013 Jun 15;56(7):347-50. doi: 10.1002/jlcr.3041. Epub 2013 Apr 2.
The development of new efficient syntheses of labeled reagents is a great challenge. Avoidance of overcomplicated procedures, availability and cost of starting materials are important considerations in choosing the synthetic route. In this report, we describe a facile and rapid preparation of labeled cyanate by ozonation of cyanide, a basic precursor. The crude cyanate was used without purification for the synthesis of various [(13)C] or [(14)C]ureidocarboxylic acids (20-68% yield from potassium cyanide). According to these results, cyanide ozonation may prove to be a promising alternative to traditional preparations of labeled cyanate.
开发新型高效的标记试剂合成方法是一项巨大的挑战。在选择合成路线时,避免程序过于复杂、起始原料的可用性和成本是重要的考虑因素。在本报告中,我们描述了一种通过对基本前体氰化物进行臭氧氧化来简便快速制备标记氰酸盐的方法。粗制氰酸盐未经纯化就用于合成各种[(13)C]或[(14)C]脲基羧酸(由氰化钾制备的产率为20 - 68%)。根据这些结果,氰化物臭氧氧化可能被证明是传统标记氰酸盐制备方法的一种有前景的替代方法。