通过微波辅助聚磷酸乙酯(PPE)促进的ω-硫代酰胺醇的闭环反应,开发了一种高效且通用的合成2-取代的噻唑啉和5,6-二氢-4 H -1,3-噻嗪的方法。环化反应涉及S N 2型机理,具有反应时间短,产率高和可预测的立体化学结果的优点。无环前体是通过改进的二酰化-硫磺化-皂化顺序,从市售的ω-氨基醇中以高收率制备的。整个过程无金属且操作简单。
Fluoroalkanosulfonyl fluorides-mediated cyclodehydration of β-hydroxy sulfonamides and β-hydroxy thioamides to the corresponding aziridines and thiazolines
An efficient method for the fluoroalkanosulfonyl fluoride-induced cyclodehydration of beta-hydroxy sulfonamides and beta-hydroxy thioamides to the corresponding aziridines and thiazolines is reported. Mild reaction conditions, operational simplicity, and high yields are the major advantages of this method. (c) 2013 Elsevier Ltd. All rights reserved.