Department of Chemistry, McMaster University, 1280 Main St. West, Hamilton, Ontario, Canada L8S 4M1.
J Org Chem. 2009 Nov 6;74(21):8133-8. doi: 10.1021/jo901475d.
A convenient method for the preparation of fluorous-tin isocyanate derivatives was developed from the corresponding acyl azides as a novel route to targeted radiopharmaceuticals that can be produced in high effective specific activity without having to resort to using HPLC. The isocyanates, which were stable for greater than 20 days when dissolved in fluorous solvents, were conjugated to a series of amines including lysine derivatives by using a variety of miscible and biphasic solvent systems where yields were consistently greater than 95%. The resulting ureas were radiolabeled with (125)I by using iodogen as the oxidant and the desired products were isolated in high radiochemical yield (>87%) and purity by using a simple fluorous solid phase extraction procedure.
一种方便的制备氟代锡异氰酸酯衍生物的方法是从相应的酰基叠氮化物发展而来的，这是一种生产靶向放射性药物的新途径，可以在不使用 HPLC 的情况下以高有效比活度生产。这些异氰酸酯在溶解于氟代溶剂中时稳定超过 20 天，然后通过使用各种混溶性和两相溶剂系统将其与一系列胺，包括赖氨酸衍生物缀合，产率始终大于 95%。所得的脲类化合物通过使用碘代反应剂作为氧化剂用 (125)I 进行放射性标记，然后通过使用简单的氟固相萃取程序，以高放射化学产率（>87%）和纯度分离出所需产物。
