公开(公告)号：US06395918B1

公开(公告)日：2002-05-28

申请号：US09697740

申请日：2000-10-27

申请人： Hans Jacob Edgar Loewenthal ,  Ron Benjamin Loewenthal

发明人： Hans Jacob Edgar Loewenthal ,  Ron Benjamin Loewenthal

IPC分类号： C07C30702

CPC分类号： C07C303/34 ,  C07B2200/07 ,  C07C303/24 ,  C07C303/26 ,  C07C305/26 ,  C07C307/02 ,  C07C309/65

摘要： The present invention provides a method of converting a hydroxy group in alcohols containing an electron withdrawing group into perfluoroalkane sulfonate and fluorosulfonate esters, which are good leaving groups, with inversion of configuration where the hydroxyl-bearing carbon is chiral. The method consists of converting an alcohol to an O—N,N-dialkylsulfamate ester and reacting it with a perfluoroalkansulfonic or fluorosulfonic acid. The method has applications in the synthesis of pharmaceutical and agrochemical compounds.

摘要翻译： 本发明提供一种将含有吸电子基团的醇的羟基转化为全氟烷基磺酸酯和氟代磺酸酯，其是具有良好离去基团的方法，其中含羟基的碳是手性反应。 该方法包括将醇转化为O-N，N-二烷基氨基磺酸酯并使其与全氟烷基磺酸或氟磺酸反应。 该方法在药物和农药化合物的合成中具有应用。